A simple and efficient approach for the synthesis of 2-aminated quinazoline derivatives via metal free oxidative annulation. Issue 13 (29th March 2017)

• Record Type: Journal Article
• Authors: Pandya, Amit N.; Villa, Eric M.; North, E. Jeffrey
• Is Part Of: Tetrahedron letters. Volume 58:Issue 13(2017)
• Page Start: 1276
• Page End: 1279
• Publication Date: 2017-03-29
• Subjects: Quinazolines -- Oxidative annulation -- Metal free -- Heteroaromatic; Chemistry, Organic -- Periodicals; 547.005
• DOI: 10.1016/j.tetlet.2017.02.033
• Languages: English
• ISSNs: 0040-4039

Abstract

Graphical abstract: Highlights: Metal-free reaction conditions for the synthesis of 2-aminoquinazolines. Mild reaction conditions for the synthesis of 2-aminoquinazolines. Functionalization of the biologically relevant quinazoline scaffold. Scalable synthesis for 2-aminoquinazolines. Abstract: A simple and efficient approach for the synthesis of 2-aminoquinazoline derivatives in moderate to good yields. This reaction employs mild reaction conditions, is metal-free and utilizes readily available starting materials making it a more viable reaction for scale up synthesis and ligand diversity. Notably, this methodology allows for the synthesis of 2-aminoquinazolines using a free amine or cyclic amine enabling structural diversity and good atom economy.