An improved process of separation of  R‐  and  S ‐timolol | Zendy

VárkonyiSchlovicskó Erika | Zendy; Takács Kálmán | Zendy; Hermecz István | Zendy

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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.

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