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An improved process of separation of R- and S-timolol

✍ Scribed by Erika Várkonyi-Schlovicskó; Kálmán Takács; István Hermecz

Publisher
Journal of Heterocyclic Chemistry
Year
1997
Tongue
English
Weight
169 KB
Volume
34
Category
Article
ISSN
0022-152X

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✦ Synopsis

Abstract

Diastereomeric timolol tartrates 4 are obtained in a one‐pot synthesis from the racemic base 2 and optically active O,O‐diacetyl‐ or O,O‐dibenzoyltartaric anhydrides 3, as only one of the diastereomers precipitates from acetone solution. Acidic hydrolysis as the corresponding 4 leads to timolol in high yield and optical purity.

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