Rapid Access to Polysubstituted Tetrahydrocarbazol‐4‐ones via Sequential Selective C—H Functionalization from N‐Nitrosoanilines

Author:

Li Chan12,Yang Yanchen3,Fang Feifei4,Liu Chaoyi256,Li Chunpu256,Wang Dechuan1,Liu Hong2356

Affiliation:

1. School of Science China Pharmaceutical University Nanjing Jiangsu 211198 China

2. State Key Laboratory of Drug Research Shanghai Institute of Materia Medica, Chinese Academy of Sciences 555 Zu Chong Zhi Road Shanghai 201203 China

3. School of Pharmacy China Pharmaceutical University Nanjing Jiangsu 211198 China

4. Lingang Laboratory Shanghai 200031 China

5. School of Pharmaceutical Science and Technology Hangzhou Institute for Advanced Study, UCAS Hangzhou Zhejiang 310024 China

6. University of Chinese Academy of Sciences Beijing 100049 China

Abstract

Comprehensive SummaryHerein, we have developed a strategy of Rh(III)‐catalyzed C—H activation of N‐nitrosoanilines and iodonium ylides to construct novel tetralydrocarbzol‐4‐one scaffolds, which provided valuable templates for sequential C—H functionalization such as alkylation, alkenylation, amidation and (hetero)arylation at C5‐position of tetralydrocarbzol‐4‐one with different coupling partners. Gram‐scale synthesis and further transformations of tetralydrocarbzol‐4‐one derivatives to Ondansetron and its analogues demonstrated the utility of this protocol, which enabled the concise and diverse construction of biologically active molecules.

Funder

National Natural Science Foundation of China

Publisher

Wiley

Subject

General Chemistry

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