Division of Medicinal and Process Chemistry, CSIR-Central Drug Research Institute, Lucknow 226001, India.
J Org Chem. 2012 Jan 20;77(2):929-37. doi: 10.1021/jo2020856. Epub 2012 Jan 9.
We have developed an efficient cyanuric chloride (2,4,6-trichloro-1,3,5-triazine, TCT) catalyzed approach for the synthesis of 2,3-dihydroquinazolin-4(1H)-one (3a-3x), 2-spiroquinazolinone (5, 7), and glycoconjugates of 2,3-dihydroquinazolin-4(1H)-one (10a, 10b) derivatives. The reaction allows rapid cyclization (8-20 min) with 10 mol % cyanuric chloride to give skeletal complexity in good to excellent yield. We believe that this novel procedure may open the door for the easy generation of new and bioactive quinazolinones.
我们开发了一种高效的三氯异氰尿酸（2,4,6-三氯-1,3,5-三嗪，TCT）催化方法，用于合成 2,3-二氢喹唑啉-4(1H)-酮（3a-3x）、2-螺喹唑啉酮（5、7）和 2,3-二氢喹唑啉-4(1H)-酮的糖缀合物（10a、10b）衍生物。该反应允许快速环化（8-20 分钟），使用 10 mol%的三氯异氰尿酸，以良好到优异的收率得到复杂的骨架。我们相信，这种新方法可能为生成新的和具有生物活性的喹唑啉酮开辟了道路。
