A Straightforward,One-Pot Protocol for the Preparation of Libraries of 2-Oxazolines

摘要

A practical protocol for the parallel synthesis of 2-oxazolines using polymer-supported reagents is described.Polymer-supported Mukaiyama reagent is used to couple a carboxylic acid with an amino alcohol,giving a beta-hydroxyamide,which is then cyclized in situ using either polymer-supported sulfonyl chloride resin or polymer-bound 2-fluoropyridinium triflate.Both 2,4-disubstituted and 2,4,5-trisubstituted 2-oxazolines are obtained in high yields and excellent purities after a simple resin filtration and solvent evaporation routine.