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    • 10. 发明申请
    • PROCESS FOR THE PREPARATION OF ANASTROZOLE
    • 制备阿那唑的方法
    • WO2006108155A3
    • 2006-11-23
    • PCT/US2006013140
    • 2006-04-06
    • SICOR INCVILLA MARCOFRETTA ROBERTADIULGHEROFF NICOLAPONTIROLI ALESSANDRO
    • VILLA MARCOFRETTA ROBERTADIULGHEROFF NICOLAPONTIROLI ALESSANDRO
    • C07D249/08A61K31/4196A61P35/00
    • C07D249/08
    • A process for preparing Anastrozole is provided. In the process the steps of a. combining 3,5-bis (2-cyanoisopropyl)toluene, a solvent selected from the group consisting of acetonitrile, dichloromethane and chlorobenzene, a brominating reagent selected from a group consisting of N-romosuccinimide and 1,3-dibromo-5,5-dimethylhydantoin, and 2,2'-azobis(2-methylpropionitrile); b. heating; c. combining with 1,2,4-triazole, a solvent selected from a group consisting of N-methylpyrrolidine, dimethylformamide, mixtures of NMP and DMF, dimethylsulfoxide, mixtures of DMSO and toluene, acetone, ACN, and tetrahydrofuran, a base selected from a group consisting of NaOH, KOH, K 2 CO 3 , and Na 2 CO 3 , and l,3-benzendiacetonitrile-5-(bromomethyl)-a, a, a, a- tetramethyl, at a temperature below -20°C are performed.
    • 提供了一种制备阿那曲唑的方法。 在这个过程中,a。 结合3,5-双(2-氰基异丙基)甲苯,选自乙腈,二氯甲烷和氯苯的溶剂,选自N-罗红琥珀酰亚胺和1,3-二溴-5,5-二氯苯的溴化试剂, 二甲基乙内酰脲和2,2'-偶氮双(2-甲基丙腈); 湾 加热; C。 与1,2,4-三唑结合,选自N-甲基吡咯烷,二甲基甲酰胺,NMP和DMF的混合物,二甲基亚砜,DMSO和甲苯的混合物,丙酮,ACN和四氢呋喃的溶剂,选自 由NaOH,KOH,K 2 CO 3 3和Na 2 CO 3 3组成的组,和1,3 - 苄基乙腈-5-(溴甲基)-a,a,a,a-四甲基,在低于-20℃的温度下进行。