1. Department of Chemistry, University of Sheffield, Sheffield, S3 7HF (UK);2. GlaxoSmithKline, Stevenage, Hertfordshire, SG1 2NY (UK)
Abstract:
A Rh‐catalyzed ortho‐amidation cyclocondensation sequence gave a range of 4‐aminoquinazolines in high yield. The method features a remarkably mild C(sp2)?H activation step and can be exploited to rapidly access compounds with established biological activity.