K. Tamazawa, H. Arima
May 1, 1984
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Journal
Journal of Labelled Compounds and Radiopharmaceuticals
Abstract
A new potent neuroleptic agent YM-09151-2, N-[(2RS, 3RS)-1-benzyl-2-methyl-3-pyrrolidinyl]-5-chloro-2-methoxy-4- (methylamino) benzamide (10c), was labeled with carbon-14 and deuterium for biochemical studies such as metabolism and 14 pharmacokinetics. The synthesis of [carbonyl-14C]YM-09151-2 (10a) from 4-amino-2-hydroxy-[carboxyl-14C] benzoic acid (1a) in six stages is described. Overall radiochemical yield was 79.1% at a specific activity of 21.18 mCi/mmol. (Methoxy-d3)YM-09151-2 (10b) was prepared from methyl 2-(methoxy-d3)-4-(N-methyl-N-tosylamido) benzoate (5b) which was obtained by the reaction of methyl 2-hydroxy-4-(N-methyl-N-tosylamido) benzoate (4c) with iodomethane-d3. Overall yield of 10b was 60.8% from iodomethane-d3.