One-pot synthesis of 3,4-dihydropyrimidin-2(1 H)-ones using chloroacetic acid as catalyst

• Published in: Bioorganic & medicinal chemistry letters Vol. 17; no. 12; pp. 3508 - 3510
• Main Authors: Yu, Yang, Liu, Di, Liu, Chunsheng, Luo, Genxiang
• Format: Journal Article
• Language: English
• Published: Oxford Elsevier Ltd 15.06.2007; Elsevier
• Subjects: Acetates - chemistry; Aldehydes - chemistry; Biginelli reaction; Calcium Channel Blockers - chemical synthesis; Calcium Channel Blockers - pharmacology; Catalysis; Chemistry; Chloroacetic acid; Dihydropyrimidinones; Exact sciences and technology; Heterocyclic compounds; Heterocyclic compounds with several n hetero atoms in the same ring, in separated rings or in fused rings; Models, Chemical; One-pot; Organic chemistry; Preparations and properties; Solvent-free; Synthesis; Thiourea - chemistry; Urea - chemistry; One-pot; Chloroacetic acid; Biginelli reaction; Dihydropyrimidinones; Synthesis; Solvent-free; One pot reaction; Catalytic reaction; Pyrimidone derivatives; Aldehyde; Thioureas; Active methylene compound; Solvent free; Pyrimidine derivatives; Ureas; Chemical synthesis
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2006.12.068

A simple and effective synthesis of 3,4-dihydropyrimidin-2(1 H)-one derivatives from aldehydes, 1,3-dicarbonyl compounds and urea or thiourea using chloroacetic acid as catalyst under solvent-free conditions is reported. A simple and effective synthesis of 3,4-dihydropyrimidin-2(1 H)-one derivatives from aldehydes, 1,3-dicarbonyl compounds and urea or thiourea using chloroacetic acid as catalyst under solvent-free conditions is described. Compared with the classical Biginelli reaction conditions, this new method has the advantage of good to excellent yields and short reaction time.