A Straightforward, One-Pot Protocol for the Preparation of Libraries of 2-Oxazolines
Journal of Combinatorial Chemistry2005Vol. 7(5), pp. 688–696
Citations Over TimeTop 22% of 2005 papers
Abstract
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.
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