Instant ligand libraries. Parallel synthesis of monodentate phosphoramidites and in situ screening in asymmetric hydrogenation

被引：86

作者：

Lefort, L ^{[1
]}

Boogers, JAF ^{[1
]}

de Vries, AHM ^{[1
]}

de Vries, JG ^{[1
]}

机构：

[1] DSM Res BV, Pharma Chem Adv Synth, Catal & Dev, NL-6160 MD Geleen, Netherlands

来源：

ORGANIC LETTERS | 2004年 / 6卷 / 11期

关键词：

D O I：

10.1021/ol049510e

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Chiral phosphoramidites have been identified as excellent ligands for various metal-catalyzed enantioselective transformations. Taking advantage of their easy preparation and modular nature, we designed a fully automated protocol for the parallel preparation of a library of 32 phosphoramidites and its screening in asymmetric hydrogenation of amino acid precursors. This initial study led to the discovery of a new ligand for the preparation of an enantiopure beta(3)-homoalanine precursor.

引用

页码：1733 / 1735

页数：3

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