Synthesis of 14C labelled heptacaine and carbisocaine, new local anaesthetics
- 1 February 1984
- journal article
- research article
- Published by Wiley in Journal of Labelled Compounds and Radiopharmaceuticals
- Vol. 21 (2) , 101-109
- https://doi.org/10.1002/jlcr.2580210203
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.Keywords
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