Toshiaki Yamaguchi | Researchain

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Journal of The Chemical Society-perkin Transactions 1 | 1990

A practical synthesis of an orally potent renin inhibitor, isopropyl (2R,3S)-4-cyclohexyl-2-hydroxy-3-{N-[(2R)-2-morpholinocarbonylmethyl-3-(1-naphthyl)propionyl]-L-histidyl}aminobutyrate

Hiromu Harada; Akira Iyobe; Atsushi Tsubaki; Toshiaki Yamaguchi; Kazuma Hirata; Tetsuhide Kamijo; Kinji Iizuka; Yoshiaki Kiso

The practical synthesis of an orally potent human renin inhibitor, isopropyl (2R,3S)-4-cyclohexyl-2-hydroxy-3-{N-[(2R)-2-morpholinocarbonylmethyl-3-(1-naphthyl)propionyl]-L-histidyl}-aminobutyrate, is presented. Optically pure cyclohexylnorstatine isopropyl ester (P1–P1′ moiety) was diastereoselectively and simply prepared from L-phenylalanine methyl ester. In a one-pot reaction, N-[(2R)-2-morpholinocarbonylmethyl-3-(1-naphthyl)propionyl]-L-histidine methyl ester (P4–P2moiety) was conveniently hydrolysed, protected with a Boc group attached to the side-chain imidazole function, and coupled with the cyclohexylnorstatine ester to give the optically pure target renin inhibitor.

Archive | 2005

Indoline compound and process for producting the same

Toshiaki Yamaguchi; Ikuo Tsuchiya; Ken Kikuchi; Takashi Yanagi

Archive | 2001

1-(3-benzyloxypropyl)-5-(2-substituted propyl) indoline derivative and method for using the same

Hiroaki Shiobara; Hideki Takeuchi; Toshiaki Yamaguchi; 寛明塩原; 敏章山口; 竹内秀樹

Archive | 2000

Method for producing optically active indoline derivative and intermediate for producing the derivative

Tetsukiyo Kamijo; Hirotaka Teranishi; Ikuo Tsuchiya; Toshiaki Yamaguchi; 哲聖上條; 依久雄土屋; 弘孝寺西; 敏章山口

Journal of Organic Chemistry | 1990

A practical synthesis of the [(2R)-3-(morpholinocarbonyl)-2-(1-naphthylmethyl)propionyl]-L-histidine moiety (P4-P2) in renin inhibitors

Hiromu Harada; Toshiaki Yamaguchi; Akira Iyobe; Atsushi Tsubaki; Tetsuhide Kamijo; Kinji Iizuka; Katsuyuki Ogura; Yoshiaki Kiso

Archive | 1998

Process for producing benzylsuccinic acid derivatives

Tetsuhide Kamijo; Toshiaki Yamaguchi; Takashi Yanagi

Archive | 1989

Acylated benzofuro[3,2-c]quinoline compounds with utility as treatments for osteoporosis

Tetsuhide Kamijo; Arao Ujiie; Hiromu Harada; Naoyuki Tsutsumi; Atsushi Tsubaki; Toshiaki Yamaguchi; Hideo Nagata

Archive | 1991

Acid addition salts of an optically active alaninanilide compound and pharmaceutical compositions containing the same

Tetsuhide Kamijo; Toshiaki Yamaguchi; Kazuhiko Ikegami

Archive | 1995

Optically active phenylbutanol derivative and its production

Tetsukiyo Kamijo; Hideki Takeuchi; Ikuo Tsuchiya; Toshiaki Yamaguchi; Takashi Yanagi; 哲聖上條; 依久雄土屋; 敏章山口; 孝志柳; 竹内秀樹

Archive | 2005

Indolinverbindung und verfahren zu deren herstellung Indoline compound and processes for their preparation

Toshiaki Yamaguchi; Ikuo Tsuchiya; Ken Kikuchi; Takashi Yanagi

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