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An Efficacious Protocol for 4‐Substituted 3,4‐Dihydropyrimidinones: Synthesis and Calcium Channel Binding Studies
Author(s) -
Singh Kamaljit,
Arora Divya,
Falkowski Danielle,
Liu Qingxin,
Moreland Robert S.
Publication year - 2009
Publication title -
european journal of organic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.825
H-Index - 155
eISSN - 1099-0690
pISSN - 1434-193X
DOI - 10.1002/ejoc.200900208
Subject(s) - chemistry , calcium channel , combinatorial chemistry , protocol (science) , calcium , organic chemistry , medicine , alternative medicine , pathology
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)