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Synthesis of [carbonyl‐14C]‐labelled remoxipride and raclopride. Two potential neuroleptic agents

 

作者: Lars Gawell,  

 

期刊: Journal of Labelled Compounds and Radiopharmaceuticals  (WILEY Available online 1986)
卷期: Volume 23, issue 1  

页码: 45-50

 

ISSN:0362-4803

 

年代: 1986

 

DOI:10.1002/jlcr.2580230106

 

出版商: John Wiley&Sons, Ltd.

 

关键词: Remoxipride;raclopride;benzamides;carbon‐14

 

数据来源: WILEY

 

摘要:

AbstractThe synthesis of two benzamide derivatives labelled with carbon‐14 at the carboxamide position is described. The radioactive label was introduced by the reaction of 1,3‐dimethoxy‐2‐lithiobenzene with [14C]carbon dioxide to furnish 2,6‐dimethoxy[carboxy‐14C]benzoic acid (2). Halogenation of2with dioxane dibromide or sulphuryl chloride followed by reaction with thionyl chloride led to the corresponding labelled acid chlorides. These were reacted with (S)‐2‐(aminomethyl)‐1‐ethylpyrrolidine (5) and converted into [14C]remoxipride (6) and [14C]racloprid

 

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