School of Pharmacy , Xinxiang Medical University , Xinxiang , Henan 453003 , P. R. China.
School of Chemistry and Chemical Engineering , Anhui University of Technology , Maanshan , Anhui 243002 , P. R. China.
Org Lett. 2019 Aug 2;21(15):6074-6078. doi: 10.1021/acs.orglett.9b02218. Epub 2019 Jul 18.
A novel method for the regioselective synthesis of 4-arylpyrimido[1,2-]indazoles has been developed via the dual C(sp)-H bond functionalization and C-N bond cleavage of triethylamine. The elusive acyclic enamine intermediates are effectively in situ generated and captured by aromatic aldehydes to form a wide array of tricyclic products from 3-aminoindazoles under the NHI-mediated aerobic oxidative conditions. This reaction features easily available feedstock, green and economic conditions, and valuable products.
一种通过三乙胺的双 C(sp)-H 键功能化和 C-N 键断裂来区域选择性合成 4-芳基嘧啶并[1,2-a]吲唑的新方法已经被开发出来。通过 NHI 介导的有氧氧化条件下，难以捉摸的非环烯胺中间体可以有效地原位生成并被芳香醛捕获，从而从 3-氨基吲唑中形成各种三环产物。该反应具有易得原料、绿色经济条件和有价值产物的特点。
