The first asymmetric synthesis of a 4-aryl-substituted 5-carboxy-3,4-dihydropyridin-2-one derivative |
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Authors: | Xiaojun Huang Jiang Zhu Scott Broadbent |
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Institution: | Chemical Synthesis, Roche Palo Alto LLC, 3431 Hillview Avenue, Palo Alto, CA 94304, USA |
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Abstract: | A simple and practical route for the asymmetric synthesis of (S)-4-(4-fluorophenyl)-1,4,5,6-tetrahydro-6-oxo-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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