Azelnidipine, CS-905, RS-9054, Calblock
阿折地平Chemical Name: (?-2-Amino-6-methyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid 3-[1-(diphenylmethyl)azetidin-3-yl] 5-isopropyl diester
CAS No. 123524-52-7, 116574-11-9 (diHCl salt, non-specified stereoch.), 116573-93-4 (non-specified sterochem.)
项目整合开发状态: Launched-2003
项目研究机构: Sankyo (Originator), Ube (Originator)
合成路线:The esterification of cyanacetic acid (I) with 1-(diphenylmethyl)azetidin-3-ol (II) by means of dicyclohexylcarbodiimide (DCC) in hot THF gives the corresponding cyanacetic ester (III),which is treated with HCl and then with NH3 to afford amidinoacetic acid (1-diphenylmethyl)azetidin-3-yl ester (IV).Finally,this compound is cyclized with 2-(3-nitrobenzylidene)acetoacetic acid isopropyl ester (V) by means of sodium methoxide in refluxing isopropanol.
📌 参考资料/链接：
参考文献标题:Dihydropyridine derivs.,their preparation and their use
文献作者:Koike,H.; Yoshimoto,M.; Nishino,H.(Sankyo Co.,Ltd.; Ube Industries,Ltd.)
参考来源:EP 0266922; EP 0529702; JP 1988253082; US 4772596
📄 详细内容
合成路线:The esterification of cyanacetic acid (I) with 1-(diphenylmethyl)azetidin-3-ol (II) by means of dicyclohexylcarbodiimide (DCC) in hot THF gives the corresponding cyanacetic ester (III),which is treated with HCl and then with NH3 to afford amidinoacetic acid (1-diphenylmethyl)azetidin-3-yl ester (IV).Finally,this compound is cyclized with 2-(3-nitrobenzylidene)acetoacetic acid isopropyl ester (V) by means of sodium methoxide in refluxing isopropanol.
参考文献标题:CS-905
文献作者:Prous,J.; Castar,J.
参考来源:Drugs Fut 1990,15(7),1671
产品链接: CAS No. 123524-52-7››