Otsuka Pharmaceutical Company, Limited

Yasuaki Muguruma

Hidenori Ogawa

Naoto Utsumi

Kaoru Abe

Shigekazu Fujita

Masahiro Miyake

Yasuhiro Torisawa

Hisayuki Tsujimori

Nobuhisa Fujita

Koichi Tsuji

Yoshihiko Okaichi

Nobuhito Tada

Daisuke Nomi

Taizo Yamaguchi

This invention provides a process for preparing benzazepine compounds of the formula (1): wherein Xis a halogen atom, Rand Rare a lower alkyl group, or salts thereof as well as intermediate benzoic acid compounds in high yield and high purity on industrial scale, which are useful as an intermediate for preparing a pharmaceutically active 2,3,4,5-tetrahydro-1H-1-benzazepine compound having vasopressin antagonistic activity.

Process for preparing benzazepine compounds or salts thereof

This invention provides a process for preparing benzazepine compounds of the formula (1): wherein Xis a halogen atom, Rand Rare a lower alkyl group, or salts thereof as well as intermediate benzoic acid compounds in high yield and high purity on industrial scale, which are useful as an intermediate for preparing a pharmaceutically active 2,3,4,5-tetrahydro-1H-1-benzazepine compound having vasopressin antagonistic activity. 

The present invention provides a process for producing 1-(3,4-dichlorobenzyl)-5-octylbiguanide or a salt thereof, the process comprising reacting 1-cyano-3-octylguanidine or a salt thereof, with 3,4-dichlorobenzylamine or a salt thereof, in an ester-based organic solvent. According to the present invention, the reaction can be carried out at a low temperature using general-purpose equipment, and 1-(3,4-dichlorobenzyl)-5-octylbiguanide or a salt thereof can be produced in a high yield by a safe and easy process.

Process for producing 1-(3,4-dichlorobenzyl)-5-octylbiguanide or a salt thereof

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Tokushima, Japan

Yasuaki Muguruma