An improved, versatile synthesis of the GABA_C antagonists (1,2,5,6-tetrahydropyridin-4-yl)methylphosphinic acid (TPMPA) and (piperidin-4-yl)methylphosphinic acid (P4MPA)

摘要

A simple, versatile and economical synthesis of the highly selective GABA_C antagonist (1,2,5,6-tetrahydropyridin-4-yl)methylphosphinic acid (TPMPA) and saturated analogue P4MPA is described. TPMPA is prepared in high yield in five steps via a palladium catalysed C-P bond forming reaction.