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TMSOTf 催化的以六甲基二硅氮烷为氮源的在无溶剂和微波辐射条件下取代的喹唑啉的合成。

TMSOTf-catalyzed synthesis of substituted quinazolines using hexamethyldisilazane as a nitrogen source under neat and microwave irradiation conditions.

机构信息

Institute of Chemistry, Academia Sinica, Taipei 115, Taiwan.

出版信息

Org Biomol Chem. 2020 Sep 23;18(36):7201-7212. doi: 10.1039/d0ob01507e.

Abstract

In this article, we report an efficient and mild synthetic route for the construction of substituted quinazolines from functionalized 2-aminobenzophenones with various benzaldehydes using cat. TMSOTf and hexamethyldisilazane (HMDS) under neat, metal-free and microwave irradiation conditions in which gaseous ammonia was formed in situ. This synthetic protocol provided the desired quinazolines with a broad substrate scope in good to excellent yields. Some structures were confirmed by X-ray single-crystal diffraction analysis.

摘要

在本文中,我们报道了一种高效、温和的合成取代喹唑啉的方法,该方法使用 TMSOTf 和六甲基二硅氮烷(HMDS),在无金属、微波辐射条件下,从功能化的 2-氨基二苯甲酮和各种苯甲醛出发,以氨气为原位形成的气体,在 neat 条件下进行反应。该合成方案提供了具有广泛底物范围的所需喹唑啉,收率良好至优秀。一些结构通过 X 射线单晶衍射分析得到证实。

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