Process for the preparation of anastrozole

Details Process for the preparation of anastrozole Process for the preparation of anastrozole

C - Chemistry, Metallurgy

07

D

C07D 249/08 (2006.01) A61K 31/4196 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2601649

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, K2CO3, and Na2CO3, and l,3-benzendiacetonitrile-5-(bromomethyl)-.alpha., .alpha., .alpha., .alpha.- tetramethyl, at a temperature below -20~C are performed.

L'invention concerne un procédé permettant de préparer anastrozole. Ledit procédé consiste: (a) à combiner 3,5-bis (2-cyanoisopropyl)toluène, un solvant choisi dans le groupe acétonitrile, dichlorométhane et chlorobenzène, un réactif de bromation choisi dans le groupe de N-bromosuccinimide et 1,3-dibromo-5,5-diméthylhydantoïne, et 2,2'- azobis(2-méthylpropionitrile); (b) à chauffer; (c) à combiner avec 1,2,4-triazole, un solvant choisi dans le groupe N-méthylpyrrolidine, diméthylformamide, des mélanges de NMP et DMF, diméthylsulfoxyde, des mélanges de DMSO et toluène, acétone, ACN, et tétrahydrofurane, une base choisie dans le groupe de NaOH, KOH, K2CO3, et Na2CO3, et 1,3-benzendiacétonitrile-5- (bromométhyl)-a, .alpha., .alpha.', .alpha.'-tétraméthyl, à une température inférieure à 20 °C.

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