201. Azido-type-selective triazole formation by iridium-catalyzed cycloaddition with thioalkynes.

K. Sugiyama, Y. Sakata, T. Niwa, S. Yoshida, *T. Hosoya
Chem. Commun., 58 (xx), xxx–xxx (2022).

200. Synthesis of Multisubstituted Benzenes from Phenols via Multisubstituted Benzynes.

A. Nagai, A. Kobayashi, Y. Sakata, Y. Minami, K. Uchida, T. Hosoya, *S. Yoshida
Synthesis, xx, xxxx (2022).

199. Computational Study for Amino Acid Production from Carboxylic Acid via 14C β-decay.

*T. Fukuchi, T. Niwa, T. Hosoya, Y. Watanabe
J. Phys. Soc. Jpn., 91 (6), 064301 (2022).

198. Expression and purification of DYRK1A kinase domain in complex with its folding intermediate-selective inhibitor FINDY.

N. Kimura, K. Saito, T. Niwa, M. Yamanaka, S. Igaue, J. Ohkanda, T. Hosoya, *I. Kii
Protein Expres. Purif. 195–196, 106089 (2022).

197. Modular synthesis of triazoles from 2-azidoacrylamides having a nucleophilic amino group.

H. Takemura, G. Orimoto, A. Kobayashi, T. Hosoya, *S. Yoshida
Org. Biomol. Chem. 20 (xx), xx–xx (2022).

196. Hydride reduction of o-(fluorosilyl)benzodifluorides for subsequent C–F transformations.

R. Idogawa, A. Kobayashi, Y. Kim, K. Shimomori, T. Hosoya, *S. Yoshida
Chem. Commun. 58 (21), 3521–3524 (2022).

195. Clinical evaluation of [18F]pitavastatin for quantitative analysis of hepatobiliary transporter activity.

T. Nakaoka, K. Kaneko, S. Irie, A. Mawatari, A. Igesaka, Y. Uetake, H. Ochiai, T. Niwa, E. Yamano, Y. Wada, M. Tanaka, K. Kotani, H. Kawahata, J. Kawabe, Y. Miki, H. Doi, T. Hosoya, K. Maeda, H. Kusuhara, Y. Sugiyama, *Y. Watanabe
Drug Metab. Pharmacok. 44, 100449 (2022).

194. Formation of Coelenteramine from 2-peroxycoelenterazine in the Ca2+-binding Photoprotein Aequorin.

*S. Inouye, M. Nakamura, T. Hosoya
Photochem. Photobiol. 98 (xx), xxxx–xxxx (2022).

193. Enzymatic conversion of dehydrocoelenterazine to coelenterazine using FMN-bound flavin reductase of NAD(P)H:FMN oxidoreductase.

*S. Inouye, M. Nakamura, T. Hosoya
Biochem. Biophys. Res. Commun. 587, 24–28 (2022).

192. Structure-activity relationship for the folding intermediate-selective inhibition of DYRK1A.

Y. Miyazaki, M. Kikuchi, K. Umezawa, A. Descamps, D. Nakamura, G. Furuie, T. Sumida, K. Saito, N. Kimura, T.
Niwa, Y. Sumida, T. Umehara, T. Hosoya, *I. Kii
Eur. J. Med. Chem. 227, 113948 (2022).

191. 3-Azidoarynes: Generation and Regioselective Reactions.

J. Taguchi, K. Kimura, K. Igawa, K. Tomooka, *T. Hosoya
Chem. Lett. 51 (2), 94–98 (2022).

190. PET imaging of brain aromatase in humans and rhesus monkeys by 11C-labeled cetrozole analogs.

K. Takahashi, *T. Hosoya, K. Onoe, T. Mori, S. Tazawa, A. Mawatari, Y. Wada, Y.Watanabe, H. Doi, *Y. Watanabe
Sci. Rep., 11, 23623 (2021).

189. Lewis acid-mediated Suzuki–Miyaura cross-coupling reaction.

*T. Niwa, *Y. Uetake, M. Isoda, T. Takimoto, M. Nakaoka, D. Hashizume, H. Sakurai, T. Hosoya
Nat. Catal., 4 (12), 1080–1088 (2021).

188. Synthesis of Azidoanilines by the Buchwald−Hartwig Amination.

Y. Sakata, S. Yoshida, *T. Hosoya
J. Org. Chem., 86 (21), 15674–15688 (2021).

187. Direct 3-Acylation of Indolizines by Carboxylic Acids for the Practical Synthesis of Red Light-Releasable Caged Carboxylic Acids.

*K. Watanabe, N. Terao, T. Niwa, *T. Hosoya
J. Org. Chem., 86 (17), 11822–11834 (2021).

186. Thioxanthone Synthesis from Benzoic Acid Esters through Directed ortho-Lithiation.

A. Kobayashi, T. Matsuzawa, T. Hosoya, *S. Yoshida
Chem. Lett., 50 (9), 1624–1627 (2021).

185. Nucleophilic transformations of azido-containing carbonyl compounds via protection of azido group.

T. Aimi, T. Meguro, A. Kobayashi, *T. Hosoya, *S. Yoshida
Chem. Commun., 57 (49), 6062–6065 (2021).

184. Chiral deaza-coelenterazine analogs for probing a substrate-binding site in the Ca2+-binding
photoprotein aequorin.

*S. Inouye, Y. Sumida, Y. Tomabechi, J. Taguchi, M. Shirouzu, *T Hosoya
PLoS One, 16 (6), e0251743 (2021).

183. Facile Synthetic Methods for Diverse N-Arylphenylalanine Derivatives via Transformations of Aryne Intermediates and Cross-Coupling Reactions.

T. Kobayashi, T. Hosoya, *S. Yoshida
Bull. Chem. Soc. Jpn., 94 (7), 1823–1832 (2021).

https://chembiolab.sakura.ne.jp/Publication.html

182. Palladium-Catalyzed Sulfinylation of Aryl- and Alkenylborons with Sulfinate Esters.

M. Suzuki, K. Kanemoto, Y. Nakamura, T. Hosoya, *S. Yoshida
Org. Lett., 23 (6), 3893–3797 (2021).

181. Transition-Metal-Free Synthesis of N-Arylphenothiazines through an N- and S-Arylation Sequence.

T. Matsuzawa, T. Hosoya, *S. Yoshida
Org. Lett., 23 (6), 2347–2352 (2021).

180. Acylalkylation of Arynes Generated from o-Iodoaryl Triflates with Hydrosilanes and Cesium Fluoride.

M. Minoshima, K. Uchida, Y. Nakamura, T. Hosoya, *S. Yoshida
Org. Lett., 23 (5), 1868–1873 (2021).

179. Diverse diaryl sulfide synthesis through consecutive aryne reactions.

H. Nakajima, Y. Hazama, Y. Sakata, K. Uchida, T. Hosoya, *S. Yoshida
Chem. Commun., 57 (21), 2621–2624 (2021).

178. Convergent Synthesis of Fluoroalkenes Using a Dual-Reactive Unit.

M. Isoda, Y. Uetake, T. Takimoto, J. Tsuda, *T. Hosoya, *T. Niwa
J. Org. Chem., 86 (2), 1622–1632 (2021).

177. Assembly of four modules onto a tetraazide platform by consecutive 1,2,3-triazole formations.

*S. Yoshida, Y. Sakata, Y. Misawa, T. Morita, T. Kuribara, H. Ito, Y. Koike, I. Kii, *T. Hosoya
Chem. Commun., 57 (7), 899–902 (2021).

176. S1PR3–G12-biased agonist ALESIA targets cancermetabolism and promotes glucose starvation.

*M. Toyomoto, A. Inoue, K. Iida, M.Denawa, I. Kii, F. M. N. Kadji, T. Kishi, D. Im, T. Shimamura, H. Onogi, S. Yoshida, S. Iwata, J. Aoki, T. Hosoya, *M. Hagiwara
Cell Chem. Biol., 28 (8), 1132–1144 (2021).

175. Facile Synthesis of Tetraarylpyrazines by Sequential Cross-coupling Approach.

Y. Nishiyama, K. Akiyama, Y. Sakata, T. Hosoya, *S. Yoshida
Chem. Lett., 50 (1), 180–183 (2021).

174. 2-Azidoacrylamides as compact platforms for efficient modular synthesis.

H. Takemura, S. Goto, T. Hosoya, *S. Yoshida
Chem. Commun., 56 (99), 15541–15544 (2020).

173. Single C–F Transformations of o-Hydrosilyl Benzotrifluorides with Trityl Compounds as All-in-One Reagents.

R. Idogawa, Y. Kim, K. Shimomori, T. Hosoya, *S. Yoshida
Org. Lett., 22 (23), 9292–9297 (2020).

172. Triazole formation of phosphinyl alkynes with azides through transient protection of phosphine by copper.

N. Terashima, Y. Sakata, T. Meguro, T. Hosoya, *S. Yoshida
Chem. Commun., 56 (90), 14003–14006 (2020).

171. Synthesis of Functionalized Benzopyran/Coumarin-Derived Aryne Precursors and Their Applications.

Y. Nakamura, Y. Sakata, T. Hosoya, *S. Yoshida
Org. Lett., 22 (21), 8505–8510 (2020).

170. Therapeutics potentiating microglial p21-Nrf2 axis can rescue neurodegeneration caused by neuroinflammation.

*A. Nakano-Kobayashi, A. Fukumoto, A. Morizane, D. T. Nguyen, T. M. Le, K. Hashida, T. Hosoya, R. Takahashi, J. Takahashi, O. Hori, *M. Hagiwara
Sci. Adv., 6 (46), eabc1428 (2020).

169. One-step synthesis of benzo[b]thiophenes by aryne reaction with alkynyl sulfides.

T. Matsuzawa, T. Hosoya, *S. Yoshida
Chem. Sci., 11 (35), 9691–9696 (2020). 日刊工業新聞 "東京医科歯科大、ベンゾチオフェン環をワンステップ合成"

168. (Hexafluoroacetylacetonato)copper(I)–cycloalkyne complexes as protected cycloalkynes.

N. Makio, Y. Sakata, T. Kuribara, K. Adachi, Y. Hatakeyama, T. Meguro, K. Igawa, K, Tomooka, T. Hosoya, *S. Yoshida
Chem. Commun., 56 (77), 11449–11452 (2020).

167. Boracene-Based Alkylborate Enabling Ni/Ir Hybrid Catalysis.

Y. Sato, Y. Miyamoto, *Y. Sumida, T. Hosoya, *H. Ohmiya
Org. Biomol. Chem., 18 (34), 6598–6601 (2020).

166. Synthesis of Dibenzofurans by Cu-Catalyzed Deborylative Ring Contraction of Dibenzoxaborins

*Y. Sumida, R. Harada, T. Sumida, K. Johmoto, H. Uekusa, *T. Hosoya
Org. Lett., 22 (16), 6687–6691 (2020).

165. Identification of a novel oxidation product from yellow fluorophore in the complex of apoPholasin and dehydrocoelenterazine.

*S. Inouye, M. Nakamura, J. Taguchi, T. Hosoya
Bioorg. Med. Chem. Lett., 30 (19), 127435 (2020).

164. Quantification of aromatase binding in the female human brain using [11C]cetrozole PET.

M. Jonasson, P. Nordeman, J. Eriksson, H. Wilking, J. Wikström, K. Takahashi, T. Niwa, T. Hosoya, Y. Watanabe, G. Antoni, I. S. Poromaa, *M. Lubberink, *E. Comasco
J. Neurosci. Res., 98 (11), 2208–2218 (2020).

163. Selective strain-promoted azide–alkyne cycloadditions through transient protection of bicyclo[6.1.0]nonynes with silver or gold.

K. Adachi, T. Meguro, Y. Sakata, K. Igawa, K, Tomooka, T. Hosoya, *S. Yoshida
Chem. Commun., 56 (68), 9823–9826 (2020).

162. Indolizines Enabling Rapid Uncaging of Alcohols and Carboxylic Acids by Red Light-Induced Photooxidation.

*K. Watanabe, N. Terao, I. Kii, R. Nakagawa, T. Niwa, *T. Hosoya
Org. Lett., 22 (14), 5434–5438 (2020).

161. Synthesis of multisubstituted cycloalkenes through carbomagnesiation of strained cycloalkynes

Y. Tamura, Y. Minami, Y. Nishiyama, Y. Sakata, F. Karaki, T. Hosoya, *S. Yoshida
Chem. Commun., 56 (52), 7147–7150 (2020).

160. Generation of Alkyl Radical through Direct Excitation of Boracene-based Alkylborate.

Y. Sato, K. Nakamura, *Y. Sumida, D. Hashizume, *T. Hosoya, *H. Ohmiya
J. Am. Chem. Soc., 142 (22), 9938–9943 (2020).[Press release(金沢大・理研・医科歯科大共同)]

159. One-pot Synthesis of Allyl Sulfides from Sulfinate Esters and Allylsilanes through Reduction of Alkoxysulfonium Intermediates

A. Kobayashi, T. Matsuzawa, T. Hosoya, *S. Yoshida
Chem. Lett., 49 (7), 813–816 (2020).

158. Aryne Reaction and Cross-Coupling Approach for the Synthesis of Diverse N-Arylphenylalanine Derivatives

T. Kobayashi, T. Hosoya, *S. Yoshida
Chem. Lett., 49 (7), 809–812 (2020).

157. Synthesis of Diverse Aromatic Ketones through C–F Cleavage of Trifluoromethyl Group

M. Ikeda, T. Matsuzawa, T. Morita, T. Hosoya, *S, Yoshida
Chem. Eur. J., 26 (54), 12333-12337 (2020).

156. Synthesis of benzyl sulfides via substitution reaction at the sulfur of phosphinic acid thioesters.

Y. Nishiyama, T. Hosoya, *S. Yoshida
Chem. Commun., 56 (43), 5771–5774 (2020).

155. Practical synthesis of [18F]pitavastatin and evaluation of hepatobiliary transport activity in rats by positron emission tomography.

T. Nakaoka, Y. Uetake, K. Kaneko, T. Niwa, H. Ochiai, S. Irie, Y. Suezaki, N. Otsuka, E. Hayashinaka, Y. Wada, Y. Cui, K. Maeda, H. Kusuhara, Y. Sugiyama, T. Hosoya, *Y. Watanabe
Mol. Pharmaceutics, 17 (6), 1884–1898 (2020).

154. Sulfoxide synthesis from sulfinate esters under Pummerer-like conditions.

A. Kobayashi, T. Matsuzawa, T. Hosoya, *S. Yoshida
Chem. Commun., 56 (40), 5429–5432 (2020).

153. Synthesis of Thioxanthones through Formal C–H Thiolation of Benzoic Acid Esters and Acid-mediated Direct Cyclization.

K. Mutsuura, Y. Sakata, K. Uchida, T. Hosoya, *S. Yoshida
Chem. Lett., 49 (7), 753–756 (2020).

152. Facile assembly of three cycloalkyne-modules onto a platform compound bearing thiophene S,S-dioxide moiety and two azido groups.

T. Meguro, Y. Sakata, T. Morita, T. Hosoya, *S. Yoshida
Chem. Commun., 56 (34), 4720–4723 (2020).

151. Functionalization of a Single C–F Bond of Trifluoromethylarenes Assisted by an ortho-Silyl Group Using a Trityl‐Based All-in-One Reagent with Ytterbium Triflate Catalyst

Y. Kim, K. Kanemoto, K. Shimomori, T. Hosoya, S. Yoshida*
Chem. Eur. J., 26 (28), 6136–6140 (2020).

150. A novel yellow fluorescent protein of recombinant apoPholasin with dehydrocoelenterazine

*S. Inouye, Y. Miura-Sahara, R. Iimori, Y. Sakata, Y. Hazama, S. Yoshida, M. Nakamura, T. Hosoya
Biochem. Biophys. Res. Commun., 526 (2), 404–409 (2020).

149. Synthesis of Phenoxathiins and Phenothiazines by Aryne Reactions with Thiosulfonates.

K. Kanemoto, Y. Sakata, T. Hosoya, *S. Yoshida
Chem. Lett., 49 (5), 593–596 (2020).

148. Expression, purification, and characterization of recombinant apoPholasin.

*S. Inouye, Y. Sahara-Miura, M. Nakamura, T. Hosoya
Protein Expr. Purif., 171, 105615 (2020).

147. Consecutive Aryne Generation Strategy for the Synthesis of 1,3-Diarylpyrazoles.

T. Kobayashi, T. Hosoya, *S. Yoshida
J. Org. Chem., 85 (6), 4448–4462 (2020).

146. HaloTag-based conjugation of proteins to barcoding-oligonucleotides.

*J. Yazaki, Y. Kawashima, T. Ogawa, A. Kobayashi, M. Okoshi, T. Watanabe, S. Yoshida, I. Kii, S. Egami, M. Amagai,
T. Hosoya, K. Shiroguchi, O. Ohara,
Nucleic Acids Res., 48 (2), e8 (2020). [理研 プレスリリース]

145. Cell-based high-throughput screening identifies a chemical chaperone for preventing ER protein aggregation and proteotoxicity.

K. Kitakaze, S. Taniuchi, E. Kawano, Y. Hamada, M. Miyake, T. Kuribara, S. Yoshida, M. Oyadomari, H. Kojima, H. Kosako, T. Hosoya, *S. Oyadomari
eLife, 8, e43302 (2019).

144. Synthesis of Diverse γ-Aryl-β-ketoesters via Aryne Intermediates Generated by C–C Bond Cleavage.

K. Uchida, Y. Minami, *S. Yoshida, *T. Hosoya
Org. Lett., 21 (22), 9019–9023 (2019). [TMDU プレスリリース]

TOC_10.1021/acs.orglett.9b03418

143. Facile Synthesis of Diverse 2,6-Disubstituted Arylsilanes via Silylamination and Silylsulfanylation of Aryne
Intermediates Generated from o-Iodoaryl Triflates.

Y. Nakamura, S. Ozawa, *S. Yoshida, *T. Hosoya
Chem. Lett., 48 (11), 1296–1299 (2019).

TOC_10.1246/cl.190573

142. 3-Thioaryne Intermediates for the Synthesis of Diverse Thioarenes.

Y. Nakamura, Y. Miyata, K. Uchida, *S. Yoshida, *T. Hosoya
Org. Lett., 21 (13), 5252–5258 (2019). [TMDU プレスリリース]

TOC_10.1246/cl.190573

141. Synthesis of (2,2-Diborylvinyl)arenes by Rhodium-Catalyzed Desulfanylative gem-Diborylation of 2-Arylvinyl
Sulfides.

Y. Uetake, M. Isoda, *T. Niwa, *T. Hosoya
Org. Lett., 21 (13), 4933–4938 (2019).

TOC_10.1246/cl.190573

140. Effect of Resonance on the Clickability of Alkenyl Azides in the Strain-promoted Cycloaddition with Dibenzo-fused
Cyclooctynes.

*S. Yoshida, S. Goto, Y. Nishiyama, Y. Hazama, M. Kondo, T. Matsushita, *T. Hosoya
Chem. Lett., 48 (9) 1038–1041 (2019).

TOC_10.1246/cl.190573

139. Synthesis of Alkynyl Sulfides by Copper-Catalyzed Thiolation of Terminal Alkynes Using Thiosulfonates.

K. Kanemoto, *S. Yoshida, *T. Hosoya
Org. Lett., 21 (9), 3172–3177 (2019). [TMDU プレスリリース]

TOC_10.1246/cl.190573

138. Facile Synthesis of Diverse o-Iodoaryl Triflates from o-Silylaryl Triflates by Aluminum-mediated Desilyliodination.

*S. Yoshida, Y. Hazama, K. Kanemoto, Y. Nakamura, *T. Hosoya
Chem. Lett., 48 (7), 742–745 (2019).

TOC_10.1246/cl.190573

137. Modular Synthesis of Unsymmetrical Doubly-ring-fused Benzene Derivatives Based on a Sequential Ring
Construction Strategy Using Oxadiazinones as a Platform Molecule.

T. Meguro, S. Chen, K Kanemoto, *S Yoshida, *T. Hosoya
Chem. Lett., 48 (6), 582–585 (2019).

TOC_10.1246/cl.190573

136. A facile preparation of functional cycloalkynes via an azide-to-cycloalkyne switching approach.

*S. Yoshida, T. Kuribara, H. Ito, T. Meguro, Y. Nishiyama, F. Karaki, Y. Hatakeyama, Y. Koike, I. Kii, *T. Hosoya
Chem. Commun., 55 (24), 3556–3559 (2019). [TMDU プレスリリース]

TOC_10.1246/cl.190573

135. Divergent Synthesis of Photoaffinity Probe Candidates by Click Reactions of Azido-Substituted
Aryltrifluoromethyldiazirines.

K. Watanabe, J. Tsuda, H. Ochiai, T. Niwa, and *T. Hosoya
Heterocycles, 99 (2), 1366-1387 (2019)


134. Synthesis of Diverse 3-Azido-5-(azidomethyl)benzene Derivatives via Formal C–H Azidation and Functional Group-
Selective Transformations.

Y. Nishiyama, Y. Misawa, Y. Hazama, K. Oya, *S. Yoshida, and *T. Hosoya
Heterocycles, 99 (2), 1053-1072 (2019)

133. Ligand binding to human prostaglandin E receptor EP4 at the lipid-bilayer interface.

Y. Toyoda, K. Morimoto, R. Suno, S. Horita, K. Yamashita, K. Hirata, Y. Sekiguchi, S. Yasuda, M. Shiroishi, T. Shimizu,
Y. Urushibata, Y. Kajiwara, T. Inazumi, Y. Hotta, H. Asada, T. Nakane, Y. Shiimura, T. Nakagita, K. Tsuge, S. Yoshida,
T. Kuribara, T. Hosoya, Y. Sugimoto, N. Nomura, M. Sato, T. Hirokawa, K. Masahiro, T. Murata, K. Takayama, M. Yamamoto,
*S. Narumiya, *S. Iwata, and *T. Kobayashi
Nat. Chem. Biol., 15, 18-26 (2019).

132. Association between aromatase in human brains and personality traits.

K. Takahashi, T. Hosoya, K. Onoe, T. Takashima, M. Tanaka, A. Ishii, Y. Nakatomi, S. Tazawa, K. Takahashi, H. Doi,
Y. Wada, and *Y. Watanabe
Sci. Rep., 8, 16841; doi: 10.1038/s41598-018-35065-4 (2018)

131. Further enhancement of the clickability of doubly sterically-hindered aryl azides by para-amino substitution.

S. Yoshida, J. Tanaka, Y. Nishiyama, Y. Hazama, T. Matsushita, and *T. Hosoya
Chem. Commun., 54, 13499–13502 (2018).

[Open Access]  Selected as inside back cover.

130. Palladium(II)-mediated rapid 11C-cyanation of (hetero)arylborons
*Z. Zhang, T. Niwa, Y. Watanabe, and *T. Hosoya

Org. Biomol. Chem., 16, 7711–7716 (2018).

129. Hydrosilyl Group-directed Iridium-catalyzed peri-Selective C–H Borylation of Ring-fused (Hetero)Arene.

*Y. Sumida, R. Harada, T. Sumida, D. Hashizume, and *T. Hosoya
Chem. Lett., 47, 1251–1254 (2018).

[Open Access]  Selected as Editor’s Choice and front cover.

128. Generation of Arynes by Selective Cleavage of a Carbon–Phosphorus Bond of o-(Diarylphosphinyl)aryl Triflates
Usinga Grignard Reagent

Y. Nishiyama, S. Kamada, *S. Yoshida, and *T. Hosoya
Chem. Lett., 47, 1216–1219 (2018). [Open Access]

127. Transient Protection of Organic Azides from Click Reactions with Alkynes by Phosphazide Formation.

T. Meguro, *S. Yoshida, K. Igawa, K. Tomooka, and *T. Hosoya
Org. Lett., 20, 4126–4130 (2018). [TMDU プレスリリース]

日経産業新聞(2018年6月26日)

126. Expanding the synthesizable multisubstituted benzo[b]thiophenes via 6,7-thienobenzynes generated from
o-silylaryl triflate-type precursors

*S. Yoshida, T. Kuribara, T. Morita, T. Matsuzawa, K. Morimoto, T. Kobayashi, and *T. Hosoya
RCS Adv., 8, 21754–21758 (2018).

[Open Access] 

125. Staudinger reaction using 2,6-dichlorophenyl azide derivatives for robust aza-ylide formation applicable to
bioconjugation in living cells.

T. Meguro, N. Terashima, H. Ito, Y. Koike, I. Kii, *S. Yoshida, and *T. Hosoya
Chem. Commun., 54, 7904–7907 (2018). [TMDU プレスリリース]

[Open Access]  Selected as back cover.

124. Slow luminescence kinetics of semi-synthetic aequorin: expression, purification and structure determination of
cf3-aequorin.

*S. Inouye, Y. Tomabechi, T. Hosoya, S. Sekine, and M. Shirouzu
J. Biochem., 164, 247–255 (2018).

Selected as front cover.

123. CDK9 Inhibitor FIT-039 Suppresses Viral Oncogenes E6 and E7 and Has a Therapeutic Effect on HPV-Induced
Neoplasia.

M. Ajiro, H. Sakai, H. Onogi, M. Yamamoto, E. Sumi, T. Sawada, T. Nomura, K. Kabashima, T. Hosoya, and *M. Hagiwara
Clin. Cancer Res., 24, 4518–4528 (2018). [京大 プレスリリース]

122. Synthesis of Diverse Phenothiazines by Direct Thioamination of Arynes with S-(o-Bromoaryl)-S-methylsulfilimines
and Subsequent Intramolecular Buchwald–Hartwig Amination.

T. Matsuzawa, K. Uchida, *S. Yoshida, and *T. Hosoya
Chem. Lett., 47, 825–828 (2018).

121. Quantification of receptor activation by oxytocin and vasopressin in endocytosis-coupled bioluminescence
reduction assayusing nanoKAZ.

*I. Kii, S. Hirahara-Owada, M. Yamaguchi, T. Niwa, Y. Koike, R. Sonamoto, H. Ito, K. Takahashi, C. Yokoyama, T. Hayashi,
T. Hosoya, and Y. Watanabe
Anal. Biochem., 549, 174–183 (2018).

120. Convergent synthesis of trifunctional molecules by three sequential azido-type-selective cycloadditions.

S. Yoshida, K. Kanno, I. Kii, Y. Misawa, M. Hagiwara, and *T. Hosoya,
Chem. Commun., 54, 3705–3708 (2018). [TMDU プレスリリース]

[Open Access]  Selected as inside back cover.

119. Modified Conditions for Copper-Catalyzed ipso-Thiolation of Arylboronic Acid Esters with Thiosulfonates.

K. Kanemoto, *S. Yoshida, and *T. Hosoya,
Chem. Lett,, 47, 85–88 (2018).

118. Synthesis of Diverse o-Arylthio-Substituted Diaryl Ethers by Direct Oxythiolation of Arynes with Diaryl Sulfoxides
InvolvingMigratory O-Arylation.

T. Matsuzawa, K. Uchida, *S. Yoshida, and *T. Hosoya,
Org. Lett, 19, 5521–5524 (2017).  [TMDU プレスリリース]

Most read article of Org. Lett. in Oct.–Nov. 2017;  日経産業新聞(2017年10月13日)

117. A study on an unusual SN2 mechanism in the methylation of benzyne through nickel-complexation.

*M. Hatakeyama, Y. Sakamoto, K. Ogata, Y. Sumida, T. Sumida, T. Hosoya, and *S. Nakamura,
Phys. Chem. Chem. Phys., 19, 26926-26933 (2017).

116. Comparison of pharmacokinetics of newly discovered aromatase inhibitors by a cassette microdosing approach in
healthy Japanese subjects.

H. Kusuhara, T. Takashima, H. Fujii, T. Takashima, M. Tanaka, A. Ishii, S. Tazawa, K. Takahashi, K. Takahashi, H. Tokai,
T. Yano, M. Kataoka, A. Inano, S. Yoshida, T. Hosoya, Y. Sugiyama, S. Yamashita, T Hojo, and *Y. Watanabe,
Drug Metab. Pharmacok., 32, 293–300 (2017).

115. Construction of Condensed Polycyclic Aromatic Frameworks through Intramolecular Cycloaddition Reactions
Involving Arynes Bearing an Internal Alkyne Moiety.

*S. Yoshida, K. Shimizu, K. Uchida, Y. Hazama, K. Igawa, K. Tomooka, and *T. Hosoya,
Chem. Eur. J., 23, 15332–15335 (2017). 

114. Copper-Catalyzed Regioselective Monodefluoroborylation of Polyfluoroalkenes en Route to Diverse Fluoroalkenes.

†H. Sakaguchi, †Y. Uetake, M. Ohashi, *T. Niwa, *S. Ogoshi, and *T. Hosoya
J. Am. Chem. Soc., 139, 12855–12862 (2017)

113. Rhodium-catalyzed odorless synthesis of diaryl sulfides from borylarenes and S-aryl thiosulfonates.

K. Kanemoto, Y. Sugimura, S. Shimizu, *S. Yoshida, and *T. Hosoya
Chem. Commun., 53, 10640–10643 (2017).

[Open Access]  Selected as inside back cover.

112. Prenatal neurogenesis induction therapy normalizes brain structure and function in Down syndrome mice.

A. Nakano-Kobayashi, T. Awaya, I. Kii, Y. Sumida, Y. Okuno, S. Yoshida, T. Sumida, H. Inoue, T. Hosoya, and *M. Hagiwara
Proc. Natl. Acad. Sci. USA, 114, 10268 (2017).  [京大 プレスリリース]

ALGERNON

111. Synthesis of Unsymmetrical Tertiary Phosphine Oxides via Sequential Substitution Reaction of Phosphonic Acid
Dithioesters with Grignard Reagents

Y. Nishiyama, Y. Hazama, *S. Yoshida, and *T. Hosoya,
Org. Lett., 19, 3899–3902 (2017).  [TMDU プレスリリース]

110. Nickel-Catalyzed Reductive Cross-Coupling of Aryl Triflates and Nonaflates with Alkyl Iodides.
*Y. Sumida, T. Sumida, and *T. Hosoya,

Synthesis, 49, 3590–3601 (2017).

109. Three-Dimensional Localization of an Individual Fluorescent Molecule with Angstrom Precision.

T. Furubayashi, K. Motohashi, K. Wakao, T. Matsuda, I. Kii, T. Hosoya, N. Hayashi, M. Sadaie, F. Ishikawa, M. Matsushita,
and *S. Fujiyoshi,
J. Am. Chem. Soc., 139, 8990–8994 (2017).  [東工大 プレスリリース]

108. Facile Transformation of α,β-Unsaturated Carboxylic Acids to Alkenylboronic Esters via Rhodium-Catalyzed
Decarbonylative Borylation of α,β-Unsaturated Thioesters.

*T. Niwa, H. Ochiai, M. Isoda, and *T. Hosoya,
Chem. Lett., 46, 1315–1318 (2017). [Open Access]

   Selected as Editor’s Choce.

107. Copper-Catalyzed ipso-Borylation of Fluoroarenes.
*T. Niwa, H. Ochiai, and *T. Hosoya,

ACS Catal., 7, 4535–4541 (2017).

Most read article in ACS Catal. Jun.–Jul. 2017

106. Development of an orally available inhibitor of CLK1 for skipping a mutated dystrophin exon in Duchenne muscular
dystrophy.

Y. Sako, K. Ninomiya, Y. Okuno, M. Toyomoto, A. Nishida, Y. Koike, K. Ohe, I. Kii, S. Yoshida, N. Hashimoto, T. Hosoya,
M. Matsuo, and *M. Hagiwara,
Sci. Rep., 7, 46126; doi: 10.1038/srep46126 (2017). [Open Access]

TG-693

105. Sequential Molecular Conjugation using Thiophene S,S-Dioxides Bearing a Clickable Functional Group.

T. Meguro, *S. Yoshida, and *T. Hosoya,
Chem. Lett., 46, 1137–1140 (2017). [Open Access]

Selected as Editor’s Choce.

104. Facile Synthesis of Phthalides from Methyl ortho-Iodobenzoates and Ketones via an Iodine–Magnesium Exchange
Reaction Using a Silylmethyl Grignard Reagent


Y. Nakamura, *S. Yoshida, and *T. Hosoya,
Chem. Lett., 46, 858–861 (2017). [Open Access]

103. Enhancing the Synthetic Utility of 3-Haloaryne Intermediates by their Efficient Generation from Readily
Synthesizable ortho-Iodoaryl Triflate-type Precursors.

*S. Yoshida, A. Nagai, K. Uchida, and *T. Hosoya,
Chem. Lett., 46, 733–736 (2017). [Open Access]

102. Three-Component Coupling of Triflyloxy-Substituted Benzocyclobutenones, Organolithium Reagents, and
Arynophiles Promoted by Generation of Aryne via Carbon–Carbon Bond Cleavage.

K. Uchida, *S. Yoshida, and *T. Hosoya,
Org. Lett., 19 (5), 1184–1187 (2017). [TMDU プレスリリース]

101. Aromatic Azido-selective Reduction via the Staudinger Reaction Using Tri-n-butylphosphonium Tetrafluoroborate
with Triethylamine.

T. Meguro, *S. Yoshida, and *T. Hosoya,
Chem. Lett., 46 (4), 473–476 (2017). [Open Access]

100. Rhodium-Catalyzed Decarbonylative Borylation of Aromatic Thioesters for Facile Diversification of Aromatic
Carboxylic Acids

H. Ochiai, Y. Uetake, *T. Niwa, and *T. Hosoya,
Angew. Chem., Int. Ed., 56 (9), 2482–2486 (2017). [Open Access]

99.Facile Synthesis of Multisubstituted Benzo[b]furans via 2,3-Disubstituted 6,7-Furanobenzynes Generated
from ortho-Iodoaryl Triflate-type Precursors

T. Morita, Y. Nishiyama, *S. Yoshida, and *T. Hosoya,
Chem. Lett., 46, 118–121 (2017). [Open Access]

Selected as Editor’s Choce.

98.Facile Diversification of Simple Benzo[b]thiophenes via Thienobenzyne Intermediates

T. Morita, *S. Yoshida, M. Kondo, T. Matsushita, and *T. Hosoya,
Chem. Lett, 46, 81–84 (2017). [Open Access]

97.Reactions of Arynes with Sulfoximines: Formal Sulfinylamination vs N-Arylation.

*S. Yoshida, H. Nakajima, K. Uchida, T. Yano, M. Kondo, T. Matsushita, and *T. Hosoya
Chem. Lett., 46, 77–80 (2017). [Open Access]

96.Aryne Relay Chemistry en Route to Aminoarenes: Synthesis of 3-Aminoaryne Precursors via Regioselective
Silylamination of 3-(Triflyloxy)arynes.

*S. Yoshida, Y. Nakamura, K. Uchida, Y. Hazama, and *T. Hosoya
Org. Lett, 18, 6212–6215 (2016).

95.Stereoinversion of Stereocongested Carbocyclic Alcohols via Triflylation and Subsequent Treatment with Aqueous
N,N-Dimethylformamide.

H. Ochiai, T. Niwa, and *T. Hosoya
Org. Lett., 18, 5982–5985 (2016).

94.The mevalonate pathway regulates primitive streak formation via protein farnesylation.

T. Okamoto-Uchida, R. Yu, N. Miyamura, N. Arima, M. Ishigami-Yuasa, H. Kagechika, S. Yoshida, T. Hosoya, M. Nawa,
T. Kasama, Y. Asaoka, R. W. Alois, U. Elling, J. M. Penninger, S. Nishina, N. Azuma, and *H. Nishina,
Sci. Rep., 6, 37697; DOI:10.1038/srep37697 (2016). [Open Access] 東京医科歯科大学プレスリリース

93.Preparation of Aryne–Nickel Complexes from ortho-Borylaryl Triflates.

Y. Sumida, T. Sumida, D. Hashizume, and *T. Hosoya
Org. Lett., 18, 5600–5603 (2016).

Most read article of Org. Lett. in Nov. 2016.

92.Blood-brain barrier permeability of ginkgolide: Comparison of the behavior of PET probes 7-[18F]Fluoro- and
10-O-p-[11C]methylbenzyl ginkgolide B in monkey and rat brains.

H. Doi, K. Sato, H. Shindou, K. Sumi, H. Koyama, T. Hosoya, Y. Watanabe, S. Ishii, *H. Tsukada, K. Nakanishi, and
*M. Suzuki
Bioorg. Med. Chem., 24, 5148–5157 (2016).

91.Thiazolobenzyne: a versatile intermediate for multisubstituted benzothiazoles.

S. Yoshida, T. Yano, Y. Nishiyama, Y. Misawa, M. Kondo, T. Matsushita, K. Igawa, K. Tomooka, and *T. Hosoya
Chem. Commun., 52, 11199–11202 (2016).

Selected as inside back cover.

90.Inhibitory effect of CDK9 inhibitor FIT-039 on hepatitis B virus propagation.

T. Tanaka, K. Okuyama-Dobashi, S. Murakami, W. Chen, T. Okamoto, K. Ueda, T. Hosoya, Y. Matsuura, A. Ryo, Y. Tanaka,
M. Hagiwara, and *K. Moriishi
Antivir. Res., 133, 156–164 (2016).

FIT-039

89.Controlled Generation of 3-Triflyloxyarynes.

K. Uchida, *S. Yoshida, and *T. Hosoya
Synthesis, 48, 4099–4109 (2016).

88.Single C-F Bond Cleavage of Trifluoromethylarenes with an ortho-Silyl Group.

*S. Yoshida, K. Shimomori, Y. Kim, and *T. Hosoya
Angew. Chem., Int. Ed., 55, 10406–10409 (2016).

Selected as Hot Paper and inside cover. 東京医科歯科大学プレスリリース

87.Rhodium-Catalyzed ipso-Borylation of Alkylthioarenes via C–S Bond Cleavage.

Y. Uetake, T. Niwa, and *T. Hosoya
Org. Lett., 18, 2758–2761 (2016).

86.Synthesis of Diverse Benzotriazoles from Aryne Precursors Bearing an Azido Group via Inter- and Intramolecular
Cycloadditions.

S. Yoshida, T. Morita, and *T. Hosoya
Chem. Lett. 45, 726–728 (2016).

Selected as Editor’s Choce. [Open Access]

85.Selective inhibition of the kinase DYRK1A by targeting its folding process.

*I. Kii, Y. Sumida, T. Goto, R. Sonamoto, Y. Okuno, S. Yoshida, T. Kato-Sumida, Y. Koike, M. Abe, Y. Nonaka, T. Ikura, N. Ito,
H. Shibuya, T. Hosoya, and *M. Hagiwara
Nat. Commun. 7, 11391: doi:10.1038/ncomms11391 (2016).

FINDY

84.Cryfstal structure of nanoKAZ: the mutated 19 kDa component of Oplophorus luciferase catalyzing
the bioluminescent reaction with coelenterazine.

Y. Tomabechi, T. Hosoya, H. Ehara, S. Sekine, M. Shirouzu, and *S. Inouye
Biochem. Biophys. Res. Commun., 470 (1), 88–93 (2016).

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