Triflic Acid-Catalyzed Highly Stereoselective Friedel-Crafts Aminoalkylation of Indoles and Pyrroles

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• 作者：Mohammed Abid ; Liliana Teixeira ; Bé ; la T&ouml ; r&ouml ; k
• 刊名：Organic Letters
• 出版年：2008
• 出版时间：March 6, 2008
• 年：2008
• 卷：10
• 期：5
• 页码：933 - 935
• 全文大小：80K
• 年卷期：v.10,no.5(March 6, 2008)
• ISSN：1523-7052

文摘

<TR>A simple and efficient synthesis to both enantiomers of highly enantiomerically enriched -trifluoromethyl--(heteroaryl)-glycine derivativesvia highly stereoselective aminoalkylation of indoles and pyrroles is described. The triflic acid-catalyzed reaction of enantiomeric 3,3,3-trifluoro-pyruvate--methylbenzyl imines with indoles and pyrroles and the subsequent Pd-catalyzed hydrogenolysis of the methylbenzyl groupprovided the products in high yields and excellent enantioselectivities.