Abstract
AbstractA potent and long acting calcium antagonist YM‐09730‐5, (3S)‐1‐benzyl‐3‐pyrrolidinyl methyl (4S)‐2,6‐dimethyl‐4‐(m‐nitrophenyl)‐1,4‐dihydropyridine‐3,5‐dicarboxylate hydrochloride (7a·HCl), was labeled with carbon‐14 and deuterium. The labeled materials were prepared by either the cyclizing Michael addition of 3‐aminocrotonate (5c) to benzylidene acetoacetate (6) or the modified Hantzsch reaction using m‐nitrobenzaldehyde, aminocrotonate(5a) and acetoacetate (3b). The 14C‐labeled material (7c·HCl) was synthesized from methyl [3‐14C]acetoacetate (4c) in a 32.0% radiochemical yield, at a specific activity of 60.9 mCi/mmol. The deuterium labeled material (7b·HCl) was synthesized from 1‐benzyl‐3‐hydroxypyrrolidine‐d4 (2b) which was obtained by the reduction of succinimide (1) with LiAlD4.
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