Synthesis of 14C labelled heptacaine and carbisocaine, new local anaesthetics

Abstract
The published four step synthesis of N‐{2‐(2‐heptyloxyphenyl‐carbamoyloxy)‐ethyl}‐piperidinium chloride (5) and N‐{2‐(2‐heptyl‐oxyphenylcarbamoyloxy)‐propyl}‐diethylammonium chloride (6), which starts from o‐acetamidophenol and 1‐bromoheptane was scaled down and modified for radioisotope work. After chromatography 1064 MBq (28,7 mCi) of [heptyl‐1‐14C]heptacaine 5 and 840 MBq (22, 6 mCi) of [heptyl‐1‐14C]carbisocaine 6 were isolated. Radiochemical yields of 5 and 6 on starting 1‐bromo [1‐14C] heptane were 30% and 25%, respectively.

This publication has 4 references indexed in Scilit: