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Synthesis and characterization of 5-methyl-1-phenyl-3,4,5,6-tetrahydro-1H-2,5-benzoxazocine-1,3,4,6-13C hydrochloride (Nefopam-13C hydrochloride)

✍ Scribed by James E. Bunker; Richard A. Newmark

Publisher
John Wiley and Sons
Year
1980
Tongue
French
Weight
246 KB
Volume
17
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

Nefopam hydrochloride (I), an analgesic agent, was labelled with carbon‐13 at C‐1,3,4 and 6 positions for metabolic studies. The starting materials for the synthesis included commercially available phthalic acid‐carboxyl‐^13^C~1~ (II) and 2‐methylaminoethyl‐1,2‐^13^C~2~ alcohol. The extent of isotope enrichment was determined by nuclear magnetic resonance and mass spectroscopy. The overall yield of I was 34% from phthalic acid‐carboxyl‐^13^C.

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