Condensation reactions of guanidines with bis-electrophiles: formation of highly nitrogenous heterocycles

TETRAHEDRON

卷:69

Article

Arnold, David M.¹  LaPorte, Matthew G.¹  Anderson, Shelby M.¹  Wipf, Peter¹ 

[1] Univ Pittsburgh, Ctr Chem Methodol & Lib Dev, Pittsburgh, PA 15260 USA

关键词: Guanidines;    Pyrimidines;    Quinazolines;    Atwal-Biginelli reaction;    Screening library;   

DOI  :  10.1016/j.tet.2013.04.127

来源: Elsevier

【 摘 要 】

2-Amino-1,4-dihydropyrimidines were reacted with bis-electrophiles to produce novel fused bipyrimidine, pyrimidoaminotriazine, and pyrimidosulfonamide scaffolds. In addition, a quinazoline library was constructed using a guanidine Atwal-Biginelli reaction with 1-(quinazolin-2-yl)guanidines. The product heterocycles have novel constitutions with high nitrogen atom counts and represent valuable additions to screening libraries for the discovery of new modulators of biological targets. (C) 2013 Elsevier Ltd. All rights reserved.

【 授权许可】

Free