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t-BuOK-Catalyzed Regio- and Stereoselective Intramolecular Hydroamination Reaction Leading to Phthalazinoquinazolinone Derivatives
The Journal of Organic Chemistry ( IF 3.3 ) Pub Date : 2023-01-03 , DOI: 10.1021/acs.joc.2c02638
Ziyi Zhang 1 , Jin Wang 2 , Shenghai Guo 1 , Jing Fan 2 , Xuesen Fan 1
Affiliation  

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.

中文翻译:

t-BuOK 催化的区域选择性和立体选择性分子内氢胺化反应生成酞嗪并喹唑啉酮衍生物

我们在此报告了一种有效且实用的策略,用于通过t -BuOK 催化的官能化喹唑啉酮的分子内加氢胺化反应在极其温和的反应下制备 5 H -酞嗪基[1,2- b ]喹唑啉-8(6 H )-酮衍生物情况。多种喹唑啉酮底物具有良好的耐受性,可通过独特的 6 -exo-dig环化工艺以高产率提供相应的产品。本协议具有易于获得的起始材料、广泛的底物范围以及高区域和立体选择性的优点。
更新日期:2023-01-03
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