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A Mild and Regioselective Route to Functionalized Quinazolines
Authors:Tracy M. M. Maiden  Dr. Stephen Swanson  Dr. Panayiotis A. Procopiou  Prof. Joseph P. A. Harrity
Affiliation: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.
Keywords:amidation  cyclization  homogeneous catalysis  oxazolines  quinazolines
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