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1,1,1,3,3,3-六氟异丙醇(HFIP)通过苄醇的亲核取代促进喹唑啉酮的N-烷基化反应。

1,1,1,3,3,3-Hexafluoroisopropanol (HFIP) Promoted N-Alkylation of Quinazolinones through Nucleophilic Substitution of Benzyl Alcohols.

作者信息

Zhang Zhiguang, Zhang Xiaomin, Liu Yanmei, Wang Xu, Zhang Xiaolei

机构信息

College of Chemical and Pharmaceutical Engineering, Hebei University of Science and Technology, Shijiazhuang, 050018, China.

Hebei Research Centre of Analysis and Testing, Hebei University of Science and Technology, Shijiazhuang, 050018, China.

出版信息

J Org Chem. 2023 Oct 6;88(19):14189-14192. doi: 10.1021/acs.joc.3c01366. Epub 2023 Sep 22.

Abstract

We describe here a protocol for alkylation of quinazolinones with a series of primary or secondary alcohols under metal-free conditions. A class of quinazolinone derivatives were obtained in 31%-97% yield with good functional group tolerance. This protocol provides chemists a direct and effective way to obtain bioactive quinazolinone derivatives.

摘要

我们在此描述了一种在无金属条件下用一系列伯醇或仲醇将喹唑啉酮烷基化的方法。以31% - 97%的产率得到了一类喹唑啉酮衍生物,且官能团耐受性良好。该方法为化学家提供了一种直接有效的途径来获得具有生物活性的喹唑啉酮衍生物。

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