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A nine‐step synthesis of [14C]flupirtine maleate labeled in the pyridine ring

 

作者: Yong M. Choi,   Norbert Kucharczyk,   R. Duane Sofia,  

 

期刊: Journal of Labelled Compounds and Radiopharmaceuticals  (WILEY Available online 1987)
卷期: Volume 24, issue 1  

页码: 1-14

 

ISSN:0362-4803

 

年代: 1987

 

DOI:10.1002/jlcr.2580240102

 

出版商: John Wiley&Sons, Ltd.

 

关键词: Potassium cyanide‐14C;1,3‐Dibromopropane;Preparative Column Chromatography;ethyl 2‐amino‐6‐{[(4‐fluorophenyl)‐methyl]amino}‐3‐pyridinyl‐2,6‐14C carbamate maleate

 

数据来源: WILEY

 

摘要:

AbstractA nine‐step procedure for microscale synthesis of ethyl 2‐amino‐6‐{[(4‐fluorophenyl)methyl]amino}‐3‐pyridinyl‐2,6‐14C carbamate maleate [10], [14C]flupirtine maleate, was developed. The synthesis started with the readily avaiable and economical reagents, potassium cyanide‐14C and 1,3‐dibromopropane making the following intermediates: glutaronitrile‐14C [2], glutarimide‐14C [3], 2,6‐dichloropyridine‐2,6‐14C [4], 2,6‐dichloro‐3‐nitro‐pyridine‐2,6‐14C [5], 2‐amino‐3‐nitro‐6‐chloropyridine‐2,6‐14C [6], 2‐amino‐3‐nitro‐6‐(p‐fluorobenzylamino)pyridine‐2,6‐14C [7], 2,3‐diamino‐6‐(p‐fluoro‐benzylamino)pyridine‐2,6‐14C [8], and ethyl 2‐amino‐6‐{[4‐fluoropheny(l)‐methyl]amino}‐3‐pyridinyl‐2,6‐14C carbamic acid ester hydrochloride [9]. The overall yield was 6.3% (5.4 mCi), and the radioac

 

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