Synthesis of Solution-Phase Phosphoramidite and Phosphite Ligand Libraries and Their In Situ Screening in the Rhodium-Catalyzed Asymmetric Addition of Arylboronic Acids

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• 作者：Richard B. C. Jagt ; Patrick Y. Toullec ; Ebe P. Schudde ; Johannes G. de Vries ; Ben L. Feringa ; Adriaan J. Minnaard
• 刊名：Journal of Combinatorial Chemistry
• 出版年：2007
• 出版时间：May 2007
• 年：2007
• 卷：9
• 期：3
• 页码：407 - 414
• 全文大小：119K
• 年卷期：v.9,no.3(May 2007)
• ISSN：1520-4774

文摘

Herein, we report the automated parallel synthesis of solution-phase libraries of phosphoramidite ligandsfor the development of enantioselective catalysts. The ligand libraries are screened in situ in theasymmetric rhodium-catalyzed addition of arylboronic acids to aldehydes and imines. It is shown that thedescribed methodology results in the straightforward discovery of leads for highly efficient enantioselectivecatalysts.