发明名称 REGIOSPECIFIC SYNTHESIS OF RAPAMYCIN 42-ESTER DERIVATIVES
摘要 FIELD: chemistry. ^ SUBSTANCE: invention relates to a method for regiospecific synthesis of rapamycin 42-ester derivatives of formula , where R is ketal isopropylidene substituted with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid, linear or branched C1-C10 alkyl, which possibly contains a halogen, C2-C8 alkenyl, or phenyl, where the said method involves acylation of 42-hydroxyrapamycin with an acyl donor in the presence of lipase. The invention also relates to regiospecific preparation of rapamycin 42-ester from ketal isopropylidene substituted with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid in the presence of lipase. ^ EFFECT: increased output of the product under mild conditions. ^ 13 cl, 12 ex
申请公布号 RU2387657(C2) 申请公布日期 2010.04.27
申请号 RU20060134014 申请日期 2005.04.12
申请人 VAJET 发明人 GU DZHIANKSIN;KAJ PING;RUPPEN MARK E.
分类号 A61K47/48;A61P35/00;C07D491/14;C07D498/18;C12P17/10;C12P17/18 主分类号 A61K47/48
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