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An improved process of separation of R‐ and S ‐timolol
Author(s) -
VárkonyiSchlovicskó Erika,
Takács Kálmán,
Hermecz István
Publication year - 1997
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.5570340357
Subject(s) - chemistry , diastereomer , timolol , yield (engineering) , acetone , hydrolysis , optically active , base (topology) , organic chemistry , medicinal chemistry , nuclear chemistry , chromatography , medicine , mathematical analysis , materials science , intraocular pressure , mathematics , metallurgy , ophthalmology
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.