Abstract
AbstractRopivacaine hydrochloride monohydrate (LEA 103) is a new local anaesthetic agent which currently is under preclinical and clinical investigation. The preparation of (S)‐N‐(2,6‐[2‐methyl‐14C]dimethylphenyl)‐1‐propylpiperidine‐2‐carboxamide hydrochloride monohydrate (6, [14C]‐LEA 103) with a specific activity of 12.44 mCi/mmol is described. The key step in the synthesis is a Pd(II)‐mediated reaction of (S)‐1‐benzyloxycarbonyl‐N‐(2‐methylphenyl)‐piperidine‐2‐carboxamide (3) with [14C]methyl iodide. Also described is the preparation of compound 3 from (S)‐2‐piperidinecarboxylic acid.
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