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Application filed by Дикран КРИКОРЯН, Стоян ПАРУШЕВ, Пепа МЕЧКАРОВАfiledCriticalДикран КРИКОРЯН
Priority to BG104937ApriorityCriticalpatent/BG64485B1/en
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Publication of BG64485B1publicationCriticalpatent/BG64485B1/en
Pharmaceuticals Containing Other Organic And Inorganic Compounds
(AREA)
Abstract
The invention relates to a method for the preparation of (-)-galantamine, wherein diphenol derivatives are subjected to oxidation with phenyliodozo(III)bis(trifluoracetate) in a polar solvent at temperature ranging from 0 to -45 degrees C for 10 to 60 min. The narvedine derivative produced is protected by ethyleneglycol and the intermediate ketal is transformed into (() -narvedine having high yield by reduction with LiAlH4. Comprehensive conversion of the racemic narvedine into (()-narvedine is made by making use, as nucleus, of crystals of (-)-narvedin. The produced (-)-narvedin is reduced stereospecifically to (-)-galantamine by means of L-selectride and at subsequent treatment with hydrogen bromide thus producing the hydrogen bromide salts of the (-)-galantamine. 4 claims
BG104937A2000-11-092000-11-09Method for the preparatrion of (-)-galantamine hydrobromide
BG64485B1
(en)
The aporphine series. Part I. Developments of the Bischler–Napieralski–Pschorr synthetic method. The synthesis of (±)-iso bulbocapnine and (±)-actinodaphnine methyl ether