Expedient Lewis Acid Catalyzed Synthesis of a 3-Substituted 5-Arylidene-1-methyl-2-thiohydantoin Library
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- 作者：Brian T. Gregg ; Kathryn C. Golden ; John F. Quinn ; Dmytro O. Tymoshenko ; William G. Earley ; Dacia A. Maynard ; Dana A. Razzano ; W. Martin Rennells ; Jennifer Butcher
- 刊名：Journal of Combinatorial Chemistry
- 出版年：2007
- 出版时间：November 2007
- 年：2007
- 卷：9
- 期：6
- 页码：1036 - 1040
- 全文大小：368K
- 年卷期：v.9,no.6(November 2007)
- ISSN：1520-4774
文摘
An efficient and rapid solution phase combinatorial synthesis of a 3-substituted 5-arylidene-1-methyl-2-thiohydantoin library was developed. The salient feature for this library production procedure is the addition of the Lewis acid catalyst, indium(III) trifluoromethanesulfonate, which serves to facilitate the direct condensation of aldehydes with 3-substituted 1-methyl-2-thiohydantoins. Use of this Lewis acid catalyst has resulted in faster reaction times, higher conversions and better purity profiles for these condensation reactions as compared to traditional uncatalyzed reactions. The resulting 315 member library of 3-substituted 5-arylidene-1-methyl-2-thiohydantoin is described.