Institute of Translation Medicine, Shanghai University, Shanghai, 200444, P. R. China.
Xinhua Hospital, School of Medicine, Shanghai Jiao Tong University, Shanghai, 200092, P. R. China.
Chem Asian J. 2021 Sep 20;16(18):2618-2621. doi: 10.1002/asia.202100681. Epub 2021 Aug 3.
Visible-light-driven sulfonylation/cyclization of N-methacryloyl-2-phenylbenzoimidazoles has been successfully developed. Using commercially available sulfonyl chloride as sulfonylation reagent, a wide range of sulfonylated benzo[4,5]imidazo[2,1-a]isoquinolin-6(5H)-ones with potential antitumor activity were provided in acceptable to excellent yields. This method has the advantages of mild reaction conditions and outstanding functional group tolerance, and provides a new strategy for the development of potential antitumor lead compounds.
可见光促进的 N-丙烯酰基-2-苯基苯并咪唑的磺酰化/环化反应已被成功开发。使用商业上可用的磺酰氯作为磺酰化试剂,提供了具有潜在抗肿瘤活性的广泛的磺酰化苯并[4,5]咪唑并[2,1-a]异喹啉-6(5H)-酮,产率可接受至优秀。该方法具有反应条件温和和突出的官能团容忍度的优点,为潜在抗肿瘤先导化合物的开发提供了新策略。