期刊
ORGANIC LETTERS
卷 18, 期 8, 页码 1872-1875出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.6b00643
关键词
-
资金
- Research Grants Council of Hong Kong [CRF: C5023-14G]
- General Research Fund [PolyU 153008/14P]
- State Key Laboratory of Chirosciences
The first general palladium catalyst for the catalytic mono-alpha-arylation of aryl- and heteroarylketones with aryl mesylates and tosylates is described. The newly developed indolyl-derived phosphine ligand L7 has been identified to promote this reaction efficiently. The key to success is attributed to the enhanced steric congestion of the catalyst and effective oxidative addition of the C((Ar))-OMs bond. In the presence of Pd(OAc)(2) (0.25-2.5 mol %) and L7, selective monoarylations are achieved with ample reaction scope and product yields up to 95%. Importantly, we demonstrated the applicability of this protocol with the modification of biological phenolic compounds, rendering it amenable for functionalization of phenolic (pro)drugs.
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