发明名称 TAXANE SYNTHESIS INTERMEDIATES AND METHODS OF PREPARATION THEREOF
摘要 organic synthesis. SUBSTANCE: in a method of preparing taxane side chain precursors, cis-beta-arylglycidate derivative having general formula I: (I) with (2R,3S) configuration is converted. In formula I, Ar is aryl and R hydrocarbon radical, preferably linear or branched alkyl optionally substituted by one or several alkyl radicals, so that could be possible regio- and stereospecific single-step preparation of beta-N- alkylamide and alpha-hydroxyl or their cyclic precursors according to Ritter reaction. Direct synthesis of linear chain is accomplished by bringing cis-beta-arylglycidate derivative I into reaction with nitrile R2- CN (R2 is aryl radical) in presence of protonic acid and water to form beta-arylisoserine derivative IIa: (IIa). Invention also relates to oxazolidine and oxazolidinone derivatives and novel baccatin derivatives. EFFECT: simplified procedure. 28 cl, 29 ex
申请公布号 RU2159237(C2) 申请公布日期 2000.11.20
申请号 RU19980110071 申请日期 1996.10.25
申请人 发明人
分类号 A61K31/337;A61K31/695;C07C229/34;C07C233/87;C07D263/14;C07D263/16;C07D263/20;C07D263/24;C07D263/26;C07D303/16;C07D303/48;C07D305/14;C07D413/12;C07F7/02;C07F7/08;C07F7/18;C07F7/30;(IPC1-7):C07D305/14 主分类号 A61K31/337
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