Affiliation:
1. Center for Drug Research and Development Guangdong Pharmaceutical University Guangzhou 510006 People's Republic of China
2. The Zhongzhou Laboratory for Integrative Biology School of Pharmacy Henan University Kaifeng Henan 475004 People's Republic of China
Abstract
AbstractA method for synthesizing pyrimido[1,2‐a]indol‐4‐ol heteroarenes via a Cp*Rh(III)‐catalyzed cascade C−H activation/annulation strategy employing N‐methoxyindoleamides and isoxazolones is developed. Also, a framework of 3‐methoxy‐2,3‐dihydro‐[1,3,5]triazino[1,2‐a]indole‐4,10‐dione was successfully synthesized via a Cp*Rh‐catalyzed C−H activation/annulation/oxidation reaction between N‐(methyloxy)‐1H‐indole‐1‐carboxamide and isoxazolones. These reactions demonstrated the suitability of several substrates, compatibility with numerous functional groups, and mild reaction conditions. Preliminary mechanistic investigations have been completed.
Funder
National Natural Science Foundation of China
Guangdong Pharmaceutical University