I2/CuCl2-Copromoted Formal [4 + 1 + 1] Cyclization of Methyl Ketones, 2-Aminobenzonitriles, and Ammonium Acetate: Direct Access to 2-Acyl-4-aminoquinazolines.
J Org Chem
; 86(23): 16916-16925, 2021 12 03.
Article
em En
| MEDLINE
| ID: mdl-34753287
ABSTRACT
We herein report an I2/CuCl2-copromoted diamination of C(sp3)-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 CuCl2 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.
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01-internacional
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MEDLINE
Assunto principal:
Cetonas
Idioma:
En
Revista:
J Org Chem
Ano de publicação:
2021
Tipo de documento:
Article