UREA FUSION PROCESS FOR THE SYNTHESIS OF 3-PHENOXY-1-AZETIDINECARBOXAMIDES

摘要

AHR-474 PATENT UREA FUSION PROCESS FOR THE SYNTHESIS OF 3-PHENOXY-1-AZETIDINECARESOXAMIDES This invention relates to an improved process for the preparation of 3-phenoxy-1-azetidinecarboxamides of Formula I which are useful Formula I in the treatment of epileptic seizures. Under Forrnula I, n is 1 to 3, X is H, halogen, trifluoromethyl, C1-C4 alkyl, C1-C4 alkoxy, acetyl, or aminocarbonyl, and R is H or methyl. This process involves heating a 3-phenoxyazetidine with urea to obtain the Formula I compound. Urea is inexpensive and easily removed by washing the solid Formula I product with water.