Process for preparing optically active 3-(methylamino)-1-(2-thienyl) propan-1-ol and intermediates for preparation
AssigneeYamakawa Chemical Industry Co., Ltd.
InventorsKenichi Sakai, Rumiko Sakurai, Atsushi Yuzawa, Kaoru Hatahira
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Abstract
Disclosed is a process for commercial preparation of 3-(methylamino)-1-(2-thienyl)propan-1-ol (hereinafter abbreviated as “MMAA”) of the formula below: The process is carried out by the diastereomeric salt formation method using optically active mandelic acid or its derivatives, or an optically active tartaric acid derivative as the resolving agent. The product compound, diastereomeric satls, is useful as the intermediate for producing pharmaceuticals, such as duloxetine.
Claims7
A process for preparation of optically active 3-(methylamino)-1-(2-thienyl)propan-1-ol (herein-after abbreviated as “MMAA”), comprising:
- optical resolution of (RS)-MMAA of the formula 1 below:
- by diastereomeric salt formation method using a resolving agent selected from optically active mandelic acid, its derivatives, optically active tartaric acid and its derivatives.
(S)-MMAA•(S)-mandelic acid monohydrate of the formula below:
(S)-MMAA•(R)-α-methoxyphenylacetic acid of the formula below:
Dependencies are inferred from the claim text.