Anastrozole, ZD-1033, ICI-D1033, Arimidex
阿那曲唑Chemical Name: 2,2'-[5-(1H-1,2,4-Triazol-1-ylmethyl)-1,3-phenylene]bis(2-methylpropionitrile)
CAS No. 120511-73-1
项目整合开发状态: Launched-1995
项目研究机构: AstraZeneca (Originator), Cancer Research UK (Not Determined), Serono (Licensee)
合成路线:The reaction of alpha,alpha'-dibromomesitylene (I) with potassium cyanide by means of tetrabutylammonium bromide (TBABr) in refluxing dichloromethane water gives 2,2'-(5-methyl-1,3-phenylene)bis(acetonitrile) (II),which is methylated with methyl iodide and NaH in DMF to yield 2,2'-(5-methyl-1,3-phenylene)bis(2-methylpropionitrile) (III).The bromination of (III) with N-bromosuccinimide (NBS) and benzoyl peroxide in CCl4 affords the bromomethyl compound (IV),which is finally condensed with sodium 1,2,4-triazole (V) in DMF.
📌 参考资料/链接：
参考文献标题:(Substd.aralkyl)heterocyclic cpds
文献作者:Edwards,P.N.; Large,M.W.(AstraZeneca plc)
参考来源:AU 8816911; EP 0296749; JP 1989019067; US 4935437
📄 详细内容
合成路线:The reaction of alpha,alpha'-dibromomesitylene (I) with potassium cyanide by means of tetrabutylammonium bromide (TBABr) in refluxing dichloromethane water gives 2,2'-(5-methyl-1,3-phenylene)bis(acetonitrile) (II),which is methylated with methyl iodide and NaH in DMF to yield 2,2'-(5-methyl-1,3-phenylene)bis(2-methylpropionitrile) (III).The bromination of (III) with N-bromosuccinimide (NBS) and benzoyl peroxide in CCl4 affords the bromomethyl compound (IV),which is finally condensed with sodium 1,2,4-triazole (V) in DMF.
参考文献标题:ZD-1033
文献作者:Mealy,N.; Prous,J.; Castar,J.
参考来源:Drugs Fut 1995,20(1),30
产品链接: CAS No. 120511-73-1››