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Cu‐Catalyzed Intramolecular Amidation of Unactivated C(sp3)−H Bonds To Synthesize N‐Substituted Indolines |
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| Authors: | Fei Pan Bin Wu Dr Zhang‐Jie Shi |
| Affiliation: | 1. Beijing National Laboratory of Molecular Science (BNLMS) and Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry Education, College of Chemistry and Molecular Engineering, Peking University, Beijing, P. R. China;2. State Key Laboratory of Organometallic Chemistry, CAS, Shanghai, P. R. China |
| Abstract: | A copper‐catalyzed intramolecular amidation of unactivated C(sp3)?H bonds to construct indoline derivatives has been developed. Such an amidation proceeded well at primary C?H bonds preferred to secondary C?H bonds. The transformation owned a broad substrate scope. The corresponding indolines were obtained in good to excellent yields. N‐Formal and other carbonyl groups were suitable and were easily deprotected and transformed into methyl or long‐chained alkyl groups. Preliminary mechanistic studies suggested a radical pathway. |
| Keywords: | C− H activation copper indoline radical synthetic methods |
