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通过简单的去对称化反应高效合成一类新型手性桥联轴手性单膦配体及其在手性 Suzuki-Miyaura 偶联反应中的应用。

Highly efficient synthesis of a class of novel chiral-bridged atropisomeric monophosphine ligands via simple desymmetrization and their applications in asymmetric Suzuki-Miyaura coupling reaction.

机构信息

School of Chemistry and Chemical Engineering, Guangdong Engineering Research Center of Chiral Drugs, Sun Yat-Sen University, No. 135 Xingangxi Road, Guangzhou 510275, PR China.

出版信息

Org Lett. 2012 Apr 20;14(8):1966-9. doi: 10.1021/ol300721p. Epub 2012 Apr 6.

DOI:10.1021/ol300721p
PMID:22482994
Abstract

A series of novel chiral-bridged atropisomeric monophosphine ligands were synthesized via convenient and simple pathways. The prepared ligands, especially for ligand 7d, were found to be highly effective in the Pd-catalyzed Suzuki-Miyaura coupling reaction. The steric hindrance and electronic effect of substrates on the reactivity and enantioselectivity were explored preliminarily.

摘要

一系列新型手性桥联非对映异构体单膦配体通过简便的方法合成。所制备的配体,特别是配体 7d,在钯催化的 Suzuki-Miyaura 偶联反应中表现出很高的活性。初步探讨了底物的空间位阻和电子效应对反应活性和对映选择性的影响。

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