Ag‐Catalyzed Remote Dehydrogenative‐coupling of Unactivated C(sp3)−H Alcohols with Quinazolines for the Synthesis of δ‐Hydroxylalkyl Substituted Quinazolines in Aqueous Media

An efficient silver‐catalyzed δ‐regioselective unactivated C(sp3 )−H of free alcohols dehydrogenative coupling with quinazolines for the synthesis of δ‐hydroxylalkyl substituted quinazolines in aqueous media has been developed. Various alcohols including 1° and 2° alcohols, reacted with quinazolines through 1,5‐hydrogen‐atom transfer strategies to give the corresponding 2‐ or 4‐ δ‐hydroxylalkyl substituted quinazolines with good to excellent yields under mild reaction conditions. Notably, several substituted quinazolines and quinazolinones could be selectively dehydrogenative‐coupled with divergent free alcohols. This protocol provides a platform to access divergent functionalizations of quinazolines and quinazolinones to meet the growing needs for screening. An efficient silver‐catalyzed δ‐regioselective unactivated C(sp3 )−H of free alcohols dehydrogen‐coupling with quinazolines for the synthesis of δ‐hydroxylalkyl substituted quinazolines in aqueous medium has been developed. This protocol provides a platform to access divergent functionalizations of quinazolines and quinazolinones to meet the growing needs for screening.