A CONVENIENT METHOD FOR LIBRARY CONSTRUCTION - PARALLEL SYNTHESIS OF BETA-AMINO ESTER AND QUINOLINE DERIVATIVES IN LIQUID-PHASE USING LN(OTF)(3)-CATALYZED 3-COMPONENT REACTIONS

A convenient method for library construction in liquid phase, which is based on lanthanide triflate (Ln(OTf)(3))-catalyzed three-component r eactions, has been developed. Equimolar amounts of each component, an aldehyde, an amine, and a silyl enol ether or an alkene, react smoothl y in the presence of Ln(OTf)(3), and the work-up and purification proc esses 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 fr om products by the simple procedure. According to this method, various high-quality beta-amino ester and quinoline derivatives have been pre pared in parallel in large quantities. (C) 1998 John Wiley & Sons, Inc .