MOE Key Laboratory of Protein Sciences, School of Pharmaceutical Sciences, Tsinghua University , Beijing 100084, China.
Org Lett. 2017 Mar 3;19(5):972-975. doi: 10.1021/acs.orglett.6b03510. Epub 2017 Feb 23.
The development of an efficient method for the construction of biologically relevant sultams is described, which represents the first case of cobalt-promoted C-H/N-H functionalization of sulfonamides with allenes. This newly developed annulation reaction demonstrated good functional group tolerance and excellent regioselectivity. Both terminal monosubstituted allenes and internal disubstituted allenes can be employed to give the desired sultams in good yields. This strategy can be successfully used to build a unique sultam library with novel structural diversity.
本文描述了一种高效构建生物相关磺酰胺的方法,这代表了首例钴促进的磺酰胺与丙二烯的 C-H/N-H 官能化反应。该新发展的环化反应表现出良好的官能团耐受性和优异的区域选择性。末端单取代丙二烯和内部双取代丙二烯均可用于以良好的收率得到所需的磺酰胺。该策略可成功用于构建具有独特结构多样性的独特磺酰胺文库。