N1-Alkylated 3,4-dihydropyrimidine-2(1H)-ones: Convenient one-pot selective synthesis and evaluation of their calcium channel blocking activity.
It has been found that selective N1-alkylation of 3,4-dihydropyrimidine-2(1H)-ones can be achieved under solvent-less, mild phase transfer catalytic (PTC) conditions with tetrabutylammonium hydrogen sulfate and 50% aqueous NaOH as the catalyst and base, respectively. The procedure is tolerant to substitutional variation at key diversity points on the pyrimidinone moiety.
Singh
Kamaljit
K
Organic Synthesis Laboratory, Department of Applied Chemical Sciences and Technology, Guru Nanak Dev University, Amritsar 143 005, India.
Arora
Divya
D
Poremsky
Elizabeth
E
Lowery
Jazmyne
J
Moreland
Robert S
RS
D000478:Alkylation; D002121:Calcium Channel Blockers / Q000138:chemical synthesis* / Q000494:pharmacology; D002384:Catalysis; D006801:Humans; D011744:Pyrimidinones / Q000138:chemical synthesis* / Q000494:pharmacology*
D002121:Calcium Channel Blockers; D011744:Pyrimidinones