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    • 4. 发明申请
    • IMPROVED PROCESS FOR HIGH PURITY ANASTROZOLE
    • 改进高纯度溶胶的方法
    • WO2007105231B1
    • 2007-11-22
    • PCT/IN2007000090
    • 2007-03-08
    • SHILPA MEDICARE LTDVISHNUKANT BPUROHIT PRASHANTPAPARAO KVEERESHAPPA VEERESHAPPA
    • VISHNUKANT BPUROHIT PRASHANTPAPARAO KVEERESHAPPA VEERESHAPPA
    • C07D249/08
    • C07D249/08
    • The present invention relates to an improved process for the preparation of anastrozole having enhanced purity from crude anastrozole having isomeric impurity content up to less than 1 %. The invention also relates to a pocess comprising steps of converting (3- cyanomethyl-5-methylphenyl) acetonitrile to 2-[(3-cyanodimethylmethyl)-5-methyl phenyl]- meiliyl propiononitrile (II) by C- alkylation, which is further converted into 2-[3-halomethyl- 5-cyanodimethyl methyl)phenyl] methyl propiononitrile (Ill) by radical bromination and further to crude anastrozole by reacting (III) with sodium salt of 1,2,4-triazole, purification of the crude anastrozole by preparing its acid addition salt, generating required final anaslrozole from the acid addition salt.
    • 本发明涉及一种用于制备具有高达小于1%的异构杂质含量的粗制阿拉曲唑具有增强的纯度的阿那曲唑的改进方法。 本发明还涉及包含以下步骤的步骤:通过C-烷基化将(3-氰基甲基-5-甲基苯基)乙腈转化为2- [(3-氰基二甲基甲基)-5-甲基苯基] - 丙烯酰基丙腈(II),其进一步 通过自由基溴化转化为2- [3-卤代甲基-5-氰基二甲基甲基)苯基]甲基丙腈(III),再通过(III)与1,2,4-三唑的钠盐反应,粗制的阿那曲唑, 阿那曲唑通过制备其酸加成盐,从酸加成盐产生所需的最终阿斯苯唑。