期刊
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
卷 137, 期 2, 页码 632-635出版社
AMER CHEMICAL SOC
DOI: 10.1021/ja512029x
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资金
- NNSFC [21272225]
- State Key Laboratory of Fine Chemicals [KF 1201]
We present the enantioselective synthesis of P-stereogenic phosphinamides through Pd-catalyzed desymmetric ortho C-H arylation of diarylphosphinamides with boronic esters. The method represents the first example of the synthesis of P-stereogenic phosphorus compounds via the desymmetric C-H functionalization strategy. The reaction proceeded efficiently with a wide array of reaction partners to afford the P-stereogenic phosphinamides in up to 74% yield and 98% ee. The efficiency was further demonstrated by gram scale syntheses. Moreover, the flexible conversion of the P-stereogenic phosphinamides into various types of P-stereogenic phosphorus derivatives was also elaborated. Thus, the protocol provides a novel tool for the efficient and versatile synthesis of P-stereogenic compounds.
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