Copper-Catalyzed Regioselective C(sp3)-H Sulfonimidization of Aliphatic Cyclic Tertiary Amines [铜催化脂肪族环状叔胺的区域选择性C(sp3)-H磺酰亚胺化]

作者：Gou Q.^*; Tan Q.; Chen Q.; Tan J.; Wang K.; Xie J.

来源：Chinese Journal of Organic Chemistry, 2021, 41(11): 4459-4466.

DOI：10.6023/cjoc202106035

• Aliphatic cyclic tertiary amines
• Copper catalysis
• Regioselective
• Sulfonylformamidines

This paper reports a concise and efficient synthesis method, namely copper-catalyzed direct hydrocarbon dehydro- genation coupling of sulfonamides and aliphatic cyclic tertiary amines, to realize the highly regioselective synthesis of (E)-N-sulfonylformamidines. The reaction is accomplished without any corrosive acid or base as an additive. It tolerates a broad scope of substrates, good functional group compatibility, and generates exclusive (E)-stereoselectivity. Moreover, this utility of the protocol is successfully demonstrated in a late-stage functionalization of medicinally active molecules and gram-scale synthesis.

• 单位
  中国科学院大学; 长江师范学院