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Issue 19, 2001
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An improved, versatile synthesis of the GABAC antagonists (1,2,5,6-tetrahydropyridin-4-yl)methylphosphinic acid (TPMPA) and (piperidin-4-yl)methylphosphinic acid (P4MPA)

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Abstract

A simple, versatile and economical synthesis of the highly selective GABAC 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.

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

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Publication details

The article was received on 05 Jul 2001, accepted on 06 Aug 2001 and first published on 13 Sep 2001


Article type: Paper
DOI: 10.1039/B105989K
J. Chem. Soc., Perkin Trans. 1, 2001, 2389-2392

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

    J. R. Hanrahan, K. N. Mewett, M. Chebib, P. M. Burden and G. A. R. Johnston, J. Chem. Soc., Perkin Trans. 1, 2001, 2389
    DOI: 10.1039/B105989K

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