Patent ID: 7858808
Filing Date: 2010-12-28
Classification: A61P,C07D

Abstract:
1. A process for the preparation of an imidazoline of the formula: wherein R 1 , R 2 , R 3 and R 4 are selected from the group consisting of alkyl, acyl, aryl, aralkyl, heteroaryl containing 5 to 14 ring members, and heterocyclic containing 5 to 12 ring members; and R 5 is selected from the group consisting of hydrogen and an alkyl group, all of which are optionally substituted, which comprises: (a) reacting a reaction mixture of (1) an oxazolone of the formula: (2) a ketone of the formula: R 3 ═O; and (3) an amine of the formula: H 2 N—R 4 in the presence of trimethyl silyl chloride or an acid chloride and a solvent for the reactants in the absence of water in the presence of a non-reactive gas and at a temperature between about 0° and 100° C. to produce the imidazoline; and (b) separating the imidazoline from the reaction mixture.