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The first asymmetric synthesis of a 4-aryl-substituted 5-carboxy-3,4-dihydropyridin-2-one derivative

✍ Scribed by Xiaojun Huang; Jiang Zhu; Scott Broadbent

Publisher
Elsevier Science
Year
2010
Tongue
French
Weight
226 KB
Volume
51
Category
Article
ISSN
0040-4039

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✦ Synopsis

A simple and practical route for the asymmetric synthesis of (S)-4-(4-fluorophenyl)-1,4,5,6-tetrahydro-6oxo-3-pyridinecarboxylic acid (1) is presented. The procedure comprises catalytic desymmetrization of a meso-anhydride using a chiral thiourea organocatalyst, followed by selective formylation and cyclization.

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