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An Efficacious Protocol for 4-Substituted 3,4-Dihydropyrimidinones: Synthesis and Calcium Channel Binding Studies

✍ Scribed by Kamaljit Singh; Divya Arora; Danielle Falkowski; Qingxin Liu; Robert S. Moreland

Publisher
John Wiley and Sons
Year
2009
Tongue
English
Weight
304 KB
Volume
2009
Category
Article
ISSN
1434-193X

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✦ Synopsis

Abstract

Ethyl 1,2‐dihydro‐1,6‐dimethyl/6‐methyl‐2‐oxopyrimidine‐5‐carboxylates react with C‐nucleophiles as well as the anion of the enantiopure chiral auxiliary (1__R__,2__S__,5__R__)‐(–)‐methyl (S)‐p‐toluenesulfinate to afford 4‐substituted and enantiopure congeners of medicinally potent Biginelli dihydropyrimidinones. The calcium channel blocking activity of some of the compounds was evaluated and compared with nifedipine for their ability to relax a membrane depolarization‐induced contraction.(© Wiley‐VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2009)

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