Title:
PRODUCTION OF OPTICALLY ACTIVE BENZOTHIEPINE SALT
Document Type and Number:
Japanese Patent JP3163393
Kind Code:
B2
Abstract:
PROBLEM TO BE SOLVED: To obtain the subject compound providing an optically active benzothiepine derivative in high purity and in high yield useful as a raw material compound for a preventive and a therapeutic agent for bone diseases, by reacting a specific benzothiepine derivative with an optically active amine.
SOLUTION: A benzothiepine derivative of formula I (R is a lower alkyl) is reacted with an optically active amine. The reaction is preferably carried out by using 0.5-1.0 equivalent of the optically active amine based on the compound of formula I, blending and reacting both the compounds in methanol or tetrahydrofuran and crystallizing or recrystallizing the objective compound. The reaction temperature is 0-30°C and the reaction time is preferably 1-10 hours. A compound of formula II (R1 is a phenyl which may be replaced; R2 to R4 are each H or a lower alkyl; R5 is H, OH, etc.), especially (1R,2S)- norephedrine is preferable as the optically active amine. The objective compound is deaminated to give an optically active benzothiepine derivative.
Inventors:
Shoji Maeda
Motoki Ikeuchi
Shigeo Yabuno
Motoki Ikeuchi
Shigeo Yabuno
Application Number:
JP19360396A
Publication Date:
May 08, 2001
Filing Date:
July 23, 1996
Export Citation:
Assignee:
Takeda GmbH
International Classes:
C07D495/04; A61K31/38; A61P19/08; A61P43/00; (IPC1-7): C07D495/04
Domestic Patent References:
| JP4364179A | ||||
| JP7101951A | ||||
| JP72727A | ||||
| JP6234766A | ||||
| JP8231569A | ||||
| JP9263545A | ||||
| JP5294960A |
Attorney, Agent or Firm:
Shuichi Takahashi (2 outside)
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