发明名称 METHOD OF SYNTHESIS OF PHYSOSTIGMINE DERIVATIVES (VARIANTS)
摘要 FIELD: organic chemistry and technology. SUBSTANCE: invention relates to new methods of synthesis of compound of the general formula (I) where R - lower alkyl; R - hydrogen atom; R - lower alkyl, lower cycloalkyl; lower cycloalkyl-lower alkyl, lower bicycloalkyl, aryl or aryl-lower alkyl, or R and R form with nitrogen atom to which they are bound the group 3,4-dihydro-2(1H)-isoquinoline; X - lower alkyl, lower alkoxy, halogen atom or trifluoromethyl group; m = 0, 1 or 2. Synthesis is carried out by interaction of compound of the general formula (II) where R, X and m have values indicated above and R - lower alkyl with alkyl-lithium or alkaline metal alcoholate followed by interaction with carboxylic acid of the general formula R -COOH where R - lower alkyl and compound of the general formula (III) where R, X and m have values indicated above is obtained. Then synthesis involves interaction of reaction mass containing compound of the general formula (III) with isocyanate of the general formula R -NCO and compound of the general formula (I) where R - hydrogen atom is obtained, or compound of the general formula (IV) where R - hydrogen atom or lower alkyl in the presence of carboxylic acid of the general formula R -COOH where R has value indicated above and compound of the general formula (V) where R, R , X and m have values indicated above is obtained by contact of reaction mixture containing the compound of the general formula (V) with compound of the general formula R<SP>1</SP>R -NH where R and R have values indicated above and isolation of compound of the general formula (I). EFFECT: improved method of synthesis. 19 cl, 1 tblE
申请公布号 RU2116307(C1) 申请公布日期 1998.07.27
申请号 RU19930045705 申请日期 1993.07.20
申请人 KHEKHST MARION RASSEL INKORPOREJTED 发明人 DZHORDZH E.LII;TOMAS B.K.LII;DONNA M.BOREK
分类号 A61K31/40;A61P25/04;A61P25/28;C07D;C07D487/04;(IPC1-7):C07D487/04 主分类号 A61K31/40
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