Journal
JOURNAL OF ORGANIC CHEMISTRY
Volume 87, Issue 5, Pages 3691-3700Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.joc.1c02622
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Funding
- NSFC [21562034]
- Natural Science Foundation of Ningxia [2019AAC02002]
- Scientific Research Project of Colleges and Universities in Ningxia [NGY2018017]
- State Key Laboratory of Natural and Biomimetic Drugs, Peking University
- Discipline Project of Ningxia [NXYLXK2017A04]
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An efficient Cp*Rh(III)-catalyzed regioselective C(sp(2))-H mono- and dialkynylation of thioamides was described. This reaction was performed under mild conditions with high yields, demonstrating versatility by controlled mono- and dialkynylation. The application of this approach in late-stage functionalization of two drug molecules (Adapalene and Amoxapine) was also demonstrated.
An efficient Cp*Rh(III) catalyzed regioselective C(sp(2))-H mono- and dialkynylation of thioamides was described. This reaction was performed under mild conditions in high yields (up to 98%) with a broad substrate scope. Significantly, the versatility of this method was further demonstrated by controlled mono- and dialkynylation. Application of this protocol in the late stage functionalization of two drug molecules (Adapalene and Amoxapine) was also demonstrated.
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