An improved, versatile synthesis of the GABA(C) antagonists (1,2,5,6-tetrahydropyridin-4-yl)methylphosphinic acid (TPMPA) and (piperidin-4-yl)methylphosphinic acid (P4MPA)

A simple, versatile and economical synthesis of highly selective GABA(C) antagonist (1,2,5,6-tetrahydropyridin-4-yl)methylphosphinic acid (TPMPA) and the saturated analogue P4MPA is described. TPMPA is prepared in high yield in five steps via a palladium catalysed C-P bond forming reaction.

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Bibliographic Details
Published inPerkin 1 : an international journal of organic and bio-organic chemistry no. 19; pp. 2389 - 2392
Main Authors Hanrahan, Mewett, KN, Chebib, M, Burden, PM, Johnston, GAR
Format Journal Article
LanguageEnglish
Published CAMBRIDGE Royal Soc Chemistry 07.10.2001
Subjects
Chemistry
Chemistry, Organic
Physical Sciences
Science & Technology
RECEPTOR ANTAGONISTS
ANALOGS
AMINO-ACIDS
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Summary:A simple, versatile and economical synthesis of highly selective GABA(C) antagonist (1,2,5,6-tetrahydropyridin-4-yl)methylphosphinic acid (TPMPA) and the saturated analogue P4MPA is described. TPMPA is prepared in high yield in five steps via a palladium catalysed C-P bond forming reaction.
ISSN:1472-7781
DOI:10.1039/b105989k