Orconazole nitrate, R-15556
Chemical Name: 1-[2-(4-Chlorophenyl)-2-(2,6-dichlorobenzyloxy)ethyl]-1H-imidazole nitrate
CAS No. 66778-38-9, 22833-02-9 (free base)
项目整合开发状态: Biological Testing
项目研究机构:
合成路线:Reaction of p-chlorophenacyl bromide (I) with imidazole (II) affords 4'-chloro-2-(1-imidazolyl)acetophenone (III).Sodium borohydride reduction gives the corresponding alcohol (IV) which is then alkylated with 2,6-dichlorobenzyl chloride (V) to give orconazole (VI).Treatment of (VI) with nitric acid yield the title compound
📌 参考资料/链接：
参考文献标题:The preparation and properties of derivatives of 1-phenethyl imidazole
文献作者:Godefroi,E.F.; et al.
参考来源:J Med Chem 1969,12(5),784
📄 详细内容
合成路线:Reaction of p-chlorophenacyl bromide (I) with imidazole (II) affords 4'-chloro-2-(1-imidazolyl)acetophenone (III).Sodium borohydride reduction gives the corresponding alcohol (IV) which is then alkylated with 2,6-dichlorobenzyl chloride (V) to give orconazole (VI).Treatment of (VI) with nitric acid yield the title compound
参考文献标题:Orconazole nitrate
文献作者:Arya,V.P.
参考来源:Drugs Fut 1979,4(6),432
合成路线:Reaction of p-chlorophenacyl bromide (I) with imidazole (II) affords 4'-chloro-2-(1-imidazolyl)acetophenone (III).Sodium borohydride reduction gives the corresponding alcohol (IV) which is then alkylated with 2,6-dichlorobenzyl chloride (V) to give orconazole (VI).Treatment of (VI) with nitric acid yield the title compound
参考文献标题:
文献作者:Godefroi,E.F.; Heeres,J.(Janssen Pharmaceutica NV)
参考来源:BE 737575; DE 1940388; FR 2015913; GB 1244530; JP 76115; US 3717655; US 3839574; ZA 6905965
产品链接: CAS No. 66778-38-9››