Abstract
We report herein an efficient and practical strategy for the preparation of 5H-phthalazino[1,2-b]quinazolin-8(6H)-one derivatives through a t-BuOK-catalyzed intramolecular hydroamination reaction of functionalized quinazolinones under extremely mild reaction conditions. A variety of quinazolinone substrates are well tolerated to furnish the corresponding products in good to high yields via an exclusive 6-exo-dig cyclization process. The present protocol has the advantages of readily obtainable starting materials, broad substrate scope, and high regio- and stereoselectivity.
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