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Title:
PRODUCTION OF OPTICALLY ACTIVE D-N-PIPERONYL-2-AMINO-@(3754/24)BENZO(B)THIOPHEN-3-YL)-PROPIONYLAMIDE
Document Type and Number:
Japanese Patent JP3192791
Kind Code:
B2
Abstract:

PURPOSE: To selectively produce the subject compound useful as an intermediate for a psychotropic agent in a high yield by allowing an acylase to act on a racemic non-natural-type acylamino acid for deacylation of the L-form compound and subsequently converting it into its derivative.
CONSTITUTION: A racemic non-natural-type acylamino acid of formula I is treated with an enzyme such as an acylase to deacylate and hydrolyze its L- form compound and a non-natural-type acyl-D-amino acid of formula III is separated from a non-natural-type L-amino acid of formula II. The compound of formula III is then hyrolyzed by using an acid and the amino group of the resultant compound is protected. The protected compound is subsequently amidated by using a condensation agent, etc., and further reacted with an acid (e.g. hydrochloric acid), thus producing the objective compound of formula V. The compound of formula V is useful as a precursor of optically active D-N-piperonyl-1,2,3,4-tetrahydro-benzo [b] thieno [2,3-c@[ pyridine-3-carboamide which is a psychotropic agent acting on the central nervous system of a mammal and having an antianxiety effect and a learning improvement effect.


Inventors:
Kawakubo, Hiroshi
Application Number:
JP1993000004594
Publication Date:
July 30, 2001
Filing Date:
January 14, 1993
Export Citation:
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Assignee:
ASAHI CHEM IND CO LTD
International Classes:
A61K31/435; A61K31/381; A61P25/20; A61P25/22; C07D409/12; C07D495/04; C12P41/00; (IPC1-7): C07D409/12; C12P41/00
Attorney, Agent or Firm:
清水 猛 (外3名)