Preparation of isoquinazolines via metal-free [4 2] cycloaddition of ynamides with nitriles
Preparation of isoquinazolines via metal-free [4 2] cycloaddition of ynamides with nitriles
复制标题
炔酰胺与腈的无金属[4 2]环加成制备异喹唑啉
DOI：
10.1039/c9ob01395d
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发表时间：
2019
影响因子：
3.2
通讯作者：
Tang Yu
中科院分区：
文献类型：
--
作者：
Wu Hao;Liu Yu;He Ming xing;Wen Hao;Cao Wei;Chen Ping;Tang Yu
TfOH介导的[4 + 2]环加成反应是通过直接反应以中等至优异的产率（高达93%）以立体特异性方式实现的。采用快速有效的方法合成了烷基取代的1，2-二氢喹唑啉衍生物，具有良好的官能团耐受性，反应时间短，非对映选择性好，反应简单，收率高。
TfOH-mediated [4 + 2] cycloaddition of ynamides with nitriles to construct 1,2-dihydroquinazolines is realized by a direct reaction in moderate to excellent yields (up to 93%) in a stereospecific manner. A rapid and efficient strategy has been employed for the syntheses of alkyl-substituted 1,2-dihydroquinazoline derivatives, and it exhibits good functional group tolerance, has a short reaction time, shows excellent diastereoselectivity, and is a simple and high-yielding reaction.