Department of Chemistry, Fujian Provincial Key Laboratory of Chemical Biology, College of Chemistry and Chemical Engineering, Xiamen University, Xiamen, Fujian 361005, P. R. China.
State Key Laboratory of Bio-organic and Natural Products Chemistry, Chinese Academy of Sciences, 354 Fenglin Road, Shanghai 200032, P. R. China.
J Org Chem. 2021 Apr 2;86(7):5345-5353. doi: 10.1021/acs.joc.0c02929. Epub 2021 Mar 12.
A facile method for the preparation of 2,3-dialkyl-substituted quinazolinones from readily available -arylamides and commercial isocyanates was developed. This one-pot procedure involves the chemoselective activation of the secondary amide with TfO/2-Br-Pyr, the sequential addition of isocyanate, and cyclization. The mild reaction is general for a wide range of substrates and can be run on a gram scale.
本文开发了一种简便的方法，可从易得的芳基酰胺和商业异氰酸酯制备 2,3-二烷基取代的喹唑啉酮。此一锅法涉及用 TfO/2-Br-Pyr 选择性活化仲酰胺，随后加入异氰酸酯并环化。该温和反应对广泛的底物具有通用性，并且可以克级规模进行。
