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    • 7. 发明申请
    • PROCESSES FOR PREPARATION OF TAXANES AND INTERMEDIATES THEREOF
    • 制备TAXANES及其中间体的方法
    • WO2009137084A3
    • 2010-02-11
    • PCT/US2009002851
    • 2009-05-06
    • IVAX RES LLCTEVA PHARMACVAK LADISLAVVALIK MARTINHOLAS TOMASMALECEK JIRI
    • CVAK LADISLAVVALIK MARTINHOLAS TOMASMALECEK JIRI
    • C07D305/14
    • C07D305/14Y02P20/55
    • A paclitaxel intermediate of formula 1 : wherein R1 is acetyl, R2 is tert-butyloxycarbonyl (BOC), R3 and R4 are phenyl and R5 is 1- ethoxyethyl, is provided. Also provided are processes for preparing taxane intermediates of formula 1 comprising reacting a compound of formula 2 with a compound of formula 3 wherein, R1, R2 and R5 are independently a hydroxyl protecting group; R3 is phenyl, substituted phenyl, a straight or branched alkyl containing 1 to 12 carbon atoms, alkenyl containing 2 to 12 carbon atoms, cycloalkyl containing 4 to 15 carbon atoms, cycloalkenyl or an R6-O- group in which R6 is: phenyl, substituted phenyl group, a C1-C8 straight or branched alkyl, a C2-C8 straight or branched alkenyl group, a C3-C8 straight or branched alkynyl, a C3-C7 cycloalkyl, C4-C7 cycloalkenyl, a C7-C11 bicycloalkyl substituent, or a saturated or unsaturated nitrogen; and R4 is phenyl or a substituted phenyl group.
    • 式1的紫杉醇中间体:其中R1是乙酰基,R2是叔丁氧基羰基(BOC),R3和R4是苯基,R5是1-乙氧基乙基。 还提供了制备式1的紫杉烷中间体的方法,包括使式2的化合物与式3的化合物反应,其中R 1,R 2和R 5独立地是羟基保护基; R3是苯基,取代苯基,含有1至12个碳原子的直链或支链烷基,含有2至12个碳原子的烯
      基,含有4至15个碳原子的环烷基,环烯基或R6-O-基,其中R6是:苯基, 取代的苯基,C1-C8直链或支链烷基,C2-C8直链或支链烯基,C3-C8直链或支链炔基,C3-C7环烷基,C4-C7环烯基,C7-C11双环烷基取代基, 或饱和或不饱和氮; 并且R 4是苯基或取代的苯基。