Unprecedented Catalytic Three Component One-Pot Condensation Reaction: An Efficient Synthesis of 5-Alkoxycarbonyl- 4-aryl-3,4-dihydropyrimidin-2(1H)-ones

Autor:	Ulf H. Dolling, Daniel R. Sidler, Hu Essa H
Rok vydání:	1998
Předmět:	chemistry.chemical_classification chemistry.chemical_compound Chemistry Aryl Organic Chemistry Biginelli reaction Urea Condensation reaction Combinatorial chemistry Aldehyde Catalysis Protic solvent
Zdroj:	The Journal of Organic Chemistry. 63:3454-3457
ISSN:	1520-6904 0022-3263
Popis:	In the past decade, 4-aryl-dihydropyrimidinones 1 have emerged as the integral backbones of several calcium channel blockers, antihypertensive agents, and alpha-1 a-antagonists.1 Strategies for the synthesis of the dihydropyrimidinone nucleus have varied from one-pot to multistep approaches. Biginelli’s initial one-pot reflux of â-keto ester 2, aryl aldehyde 3, and urea, 4, with catalytic acid in a protic solvent frequently afforded low (20-50%) yields.2,3 Subsequent multistep syntheses produced somewhat higher yields but lacked the simplicity of the one-pot, one-step synthesis.3
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::53405d61319acc0e75d6071b950b83f4 https://doi.org/10.1021/jo970846u Zobrazit plný text záznamu