An improved synthesis of tiapamil 3, Ro 11-1781, N-(3,4-dimethoxyphenethyl)- 2-(3,4-dimethoxyphenyl)-N-methyl-m-dithiane-2-propylamine 1,1,3,3-tetraoxide is described. The structure of the corresponding hydrochloride monohydrate 4, a Ca++ antagonist has been confirmed by an X-ray crystallographic analysis. Since biotransformation of tiapamil into metabolites 5, 6 and 7 occurs mainly in the close vicinity of the nitrogen atom, compound 8 bearing seven deuterium atoms has been synthesised.
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