Muto K, Kuroda T, Kawato H, Nishikawa H, Nakamizo N
Pharmaceutical Research Laboratories, Kyowa Hakko Kogyo Co., Ltd., Shizuoka, Japan.
Arzneimittelforschung. 1988 Nov;38(11A):1666-70.
(+/-)-(R*)-2,6-Dimethyl-4-(m-nitrophenyl)-1,4-dihydropyridine-3, 5-dicarboxylic acid (R*)-1-benzyl-3-piperidinyl ester, methyl ester hydrochloride (benidipine hydrochloride, KW-3049, 1), a highly potent and long-acting calcium antagonistic 1,4-dihydropyridine derivative, is now under clinical study as an antihypertensive and as an antianginal agent. In order to confirm the structures of the metabolites of KW-3049, 19 compounds were prepared. Among them 11 compounds were found to be metabolites (the compounds 2, 3, 6, 8, 14, 15, 16, 28, 31, 32 and 34) of KW-3049 in rats and/or dogs.
（±）-（R*）-2,6-二甲基-4-（间硝基苯基）-1,4-二氢吡啶-3,5-二羧酸（R*）-1-苄基-3-哌啶酯甲酯盐酸盐（盐酸贝尼地平，KW-3049，1），一种高效长效的钙拮抗1,4-二氢吡啶衍生物，目前正作为抗高血压药和抗心绞痛药进行临床研究。为了确认KW-3049的代谢物结构，制备了19种化合物。其中11种化合物被发现是KW-3049在大鼠和/或狗体内的代谢物（化合物2、3、6、8、14、15、16、28、31、32和34）。
