Elisartan potassium, HN-65021
依利沙坦 依利沙坦 Chemical Name: (?-2-Butyl-4-chloro-1-[2'-(1H-tetrazol-5-yl)biphenyl-4-ylmethyl]-1H-imidazole-5-carboxylic acid 1-(ethoxycarbonyloxy)ethyl ester potassium salt
CAS No. 158682-68-9 (free acid), 149968-26-3 (undefined isomer), 149968-27-4 (undefined isomer, Na salt)
项目整合开发状态: Phase II
项目研究机构: Amersham Health (Originator)
合成路线:The esterification of 2-butyl-4-chloro-1H-imidazole-5-carboxylic acid (I) with 1-chloroethyl ethyl carbonate (II) by means of sodium silanolate in HMPT gives the corresponding ester (III),which is condensed with 5-[4'-(bromomethyl)biphenyl-2-yl]-1-(triphenylmethyl)tetrazole (IV) by means of K2CO3 in hot DMF,yielding the tritylated final product (V).Finally,this compound is deprotected in refluxing methanol.
📌 参考资料/链接：
参考文献标题:Acylals of imidazole-5-carboxylic acid derivs.,and their use as angiotensin (II) inhibitors
文献作者:Binder,D.; Weinberger,J.
参考来源:EP 0535420; US 5298519
📄 详细内容
合成路线:The esterification of 2-butyl-4-chloro-1H-imidazole-5-carboxylic acid (I) with 1-chloroethyl ethyl carbonate (II) by means of sodium silanolate in HMPT gives the corresponding ester (III),which is condensed with 5-[4'-(bromomethyl)biphenyl-2-yl]-1-(triphenylmethyl)tetrazole (IV) by means of K2CO3 in hot DMF,yielding the tritylated final product (V).Finally,this compound is deprotected in refluxing methanol.
参考文献标题:Elisartan Potassium
文献作者:Mealy,N.; Castar,J.
参考来源:Drugs Fut 1996,21(2),139
产品链接: CAS No. 158682-68-9›› 产品链接: CAS No.149968-26-3››