Process for production of 1-(3-(2-(1-benzothiophen-5-yl)-ethoxy)propyl)azetidin-3-ol or salts thereof
AssigneeToyama Chemical Co., Ltd.
InventorsAkihito Saitoh, Yoshiaki Suzuki, Kenji Yonezawa, Mitsuhide Kawamura, Takahiko Kusanagi, Takashi Nakai
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Abstract
A Process for production of 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or salts thereof which comprises using as a starting compound as a (phenylthio)acetic acid derivative or salts thereof represented by the general formula: wherein X1 represents a halogen atom, is useful as a safe process for mass production of 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or salts thereof which is useful as a remedy for disease of central and peripheral nerve.
Claims14
A process for production of 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol, a salt of 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol, or a combination thereof, the process comprising:
- (A) reducing 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propionyl)azetidin-3-ol with an activator in the presence of an alkali metal borohydride,
- wherein the activator is at least one compound selected from the group consisting of a protonic acid, a methylating agent, and a silylating agent.
Dependencies are inferred from the claim text.