Azelnidipine, CS-905, RS-9054, Calblock-药物合成数据库

【药物名称】Azelnidipine, CS-905, RS-9054, Calblock

化学结构式(Chemical Structure):

参考文献No.	8241
标题:	Dihydropyridine derivs., their preparation and their use
作者:	Koike, H.; Yoshimoto, M.; Nishino, H. (Sankyo Co., Ltd.; Ube Industries, Ltd.)
来源:	EP 0266922; EP 0529702; JP 1988253082; US 4772596

合成路线图解说明: 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No.	115361
标题:	CS-905
作者:	Prous, J.; Casta馿r, J.
来源:	Drugs Fut 1990,15(7),1671

合成路线图解说明: 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.