SYNTHESIS OF C-14-LABELED ROPIVACAINE, A LOCAL-ANESTHETIC AGENT

被引：4

作者：

SAHLBERG, C

机构：

[1] Department of Drug Metabolism, ASTRA Alab AB, Södertälje

来源：

JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 1987年 / 24卷 / 05期

关键词：

carbon‐14; labelling; local anaesthetic agent; Pd(II)‐mediated ortho‐alkylation; ropivacaine;

D O I：

10.1002/jlcr.2580240508

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

Ropivacaine 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. Copyright © 1987 John Wiley & Sons, Ltd.

引用

页码：529 / 534

页数：6

共 3 条

[1] REAGENTS AND SYNTHETIC METHODS .21. THIONYL CHLORIDE /4-(N,N-DIMETHYLAMINO)PYRIDINE COMPLEX - A SIMPLE ONE-POT METHOD FOR ESTERIFICATION OF CARBOXYLIC-ACIDS [J].