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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