Efficacious one-pot synthesis of 2-thiazolines and 2-oxazolines under solvent and metal-free conditions

Abstract

\n\n2-Oxazolines and 2-thiazolines are very important heterocycles due to their extensive applications in chemistry, biochemistry and pharmacology. Most of the precedent methods for preparing these heterocycles involve one or more drawbacks including harsh reaction conditions, long reaction times, low yields of products, high temperature and toxic solvents.\n\n\n\nA new and eco-efficient method developed for the preparation of 2-oxazolines and 2-thiazolines. \n\n\n\ncondensation of amino alcohols with nitriles in a sealed tube under solvent-free and metal-free conditions.\n\n\n\nOur procedure appears to be highly eco-efficient and promoted quantitative access to 2-oxazolines and 2-thiazolines under simple and minimum manipulation.\n\n\n\nThis simple approach allows high conversion for different nitriles yielded from 78 to 99 % and easy isolation of the targeted products without further purification. To the best of our knowledge, our procedure is the best efficient and fast method reported to date, in terms of chemical yields, number of steps and atom economy.\n\n