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A convenient method for library construction: parallel synthesis of beta-amino ester and quinoline derivatives in liquid phase using Ln(OTf)3-catalyzed three-component reactions

A convenient method for library construction in liquid phase, which is based on lanthanide triflate (Ln(OTf)3)-catalyzed three-component reactions, has been developed. Equimolar amounts of each component, an aldehyde, an amine, and a silyl enol ether or an alkene, react smoothly in the presence of Ln(OTf)3, and the work-up and purification processes are performed by simply passing through a short column. The key is to use Ln(OTf)3 as a Lewis acid catalyst, which is not decomposed during the work-up and purification steps, and is easily separated from products by the simple procedure. According to this method, various high-quality beta-amino ester and quinoline derivatives have been prepared in parallel in large quantities. Copyright 1998 John Wiley & Sons, Inc.