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#34753287   2021/11/09 To Up

I/CuCl-Copromoted Formal [4 + 1 + 1] Cyclization of Methyl Ketones, 2-Aminobenzonitriles, and Ammonium Acetate: Direct Access to 2-Acyl-4-aminoquinazolines.

We herein report an I/CuCl-copromoted diamination of C(sp)-H bonds for the preparation of 2-acyl-4-aminoquinazolines from methyl ketones, 2-aminobenzonitriles, and ammonium acetate. This reaction features operational simplicity, commercially available substrates, mild reaction conditions, and good functional group compatibility. Mechanistic studies indicate that CuCl plays a pivotal role in this transformation. This study uses a methyl group as a novel input to construct 2-acyl-4-aminoquinazoline derivatives for the first time.
Chun Huang, You Zhou, Xiao-Xiao Yu, Li-Sheng Wang, Yan-Dong Wu, An-Xin Wu

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