Facile Pd-catalyzed amination of imidazolin-1-yl chloroazines under microwave irradiation: toward a new kinase-inhibitory chemotype. Issue 21 (20th May 2015)

• Record Type: Journal Article
• Authors: Mujumdar, Prashant; Sarnpitak, Pakornwit; Shetnev, Anton; Dorogov, Mikhail; Krasavin, Mikhail
• Is Part Of: Tetrahedron letters. Volume 56:Issue 21(2015)
• Page Start: 2827
• Page End: 2831
• Publication Date: 2015-05-20
• Subjects: 2-Imidazoline -- Chemical instability -- Microwave irradiation -- Buchwald–Hartwig amination -- Kinase inhibitors -- Hinge region binders; Chemistry, Organic -- Periodicals; 547.005
• DOI: 10.1016/j.tetlet.2015.04.059
• Languages: English
• ISSNs: 0040-4039

Abstract

Graphical abstract: Abstract: The imidazolin-1-yl azine moiety, constructed using a recently developed Buchwald–Hartwig-type arylation methodology, displays excellent chemical stability under subsequent microwave-assisted Pd-catalyzed amination with a range of N -nucleophiles. This finding extends the usage of imidazolin-1-yl azines for bioactive compound library design. The latter is exemplified herein by the discovery of micromolar kinase inhibitors.