Key Laboratory of Marine Drugs, Chinese Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Yushan Road, Qingdao, 266003, P. R. China.
Org Biomol Chem. 2019 Sep 28;17(36):8408-8416. doi: 10.1039/c9ob01395d. Epub 2019 Sep 3.
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.
TfOH 介导的炔酰胺与腈的 [4 + 2] 环加成反应以立体专一的方式实现了中等至优异的收率（高达 93%）构建 1,2-二氢喹唑啉。采用快速高效的策略合成了烷基取代的 1,2-二氢喹唑啉衍生物，该方法具有良好的官能团耐受性、较短的反应时间、优异的非对映选择性，是一种简单高产的反应。
