Synthesis 2023; 55(20): 3364-3372
DOI: 10.1055/a-2147-2620
paper

Rhodium-Catalyzed C–H Activation of 2-Arylquinazolinones and Cyclization with Elemental Sulfur via C–S/S–N Bond Formation to Access 7H-Benzo[4,5]isothiazolo[3,2-b]quinazolinones

Xinqin Zhang
,
Qiong Wu
,
Qin Yang
,
Yang Fu
,
Yiyuan Peng
Financial support from National Natural Science Foundation of China (no. 21762020 and 22261027) is gratefully acknowledged.


Abstract

An efficient method for the synthesis of 7H-benzo[4,5]isothiazolo[3,2-b]quinazolin-7-ones by the reaction of 2-arylquinazolin-4(3H)-ones and elemental sulfur is described. The rhodium-catalyzed C–H activation of 2-arylquinazolinones and cyclization with elemental sulfur via one-step formation of C–S/N–S bonds to give the corresponding 7H-benzo[4,5]isothiazolo[3,2-b]quinazolinones is realized in good to high yields with good functional group tolerance.

Supporting Information



Publication History

Received: 29 May 2023

Accepted after revision: 02 August 2023

Accepted Manuscript online:
02 August 2023

Article published online:
07 September 2023

© 2023. Thieme. All rights reserved

Georg Thieme Verlag KG
Rüdigerstraße 14, 70469 Stuttgart, Germany