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Updated: Feb 26, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Synthesis of CF3/CHF2 Dihydroquinoline Sulfonyl Fluorides: A Class of Important Pharmacophores
Meili Zou1, Hao Yang1, Weiran Yang1
1School of College of Chemistry and Chemical Engineering, Nanchang University, 999 XueFu Road, Nangchang 330031, China.
Abstract:
Here, we report the modular synthesis of trifluoromethylated/difluoromethylated dihydroquinoline sulfonyl fluorides via [4 + 2] cycloadditions of o-aminotrifluoroacetophenone derivatives or o-aminodifluoroacetophenone derivatives with 2-chloroprop-2-ene-1-sulfonyl fluoride (CESF) under mild reaction conditions. Subsequent sulfur(VI) fluoride exchange was subjected to optimization for nucleophiles based on nitrogen and oxygen, furnishing sulfonamides and sulfonates, respectively. The reaction is accomplished without employing transition metal catalysts, yielding novel products that hold significant potential in the fields of medicinal chemistry, chemical biology, and drug discovery.
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