Synthesis of [14‐¹⁴C] dexclamol hydrochloride and [14‐¹⁴C] butaclamol hydrochloride

Abstract

The synthesis of two [14C] labelled compounds, dexclamol and butaclamol hydrochloride, having the octahydrobenzocyclohepta pyridoisoquinoline structure is described. Both compounds were prepared by the same synthetic route starting from silver [14C]‐cyanide and were labelled in the 14‐position. Butaclamol (specific activity 1.23 mCi/mmole) was obtained in 13% overall yield while dexclamol (specific activity 17.8 mCi/mmole), an optically active compound requiring resolution in its preparation, was obtained in 2% overall yield.