Patent ID: 6407241
Filing Date: 2002-06-18
Classification: C07D

Abstract:
A process of preparing a compound of stuctural formula (II): whereinAr is mono-or di-substituted phenyl, naphthyl, pyridyl, furyl, thienyl, pyrrolyl, oxazolyl, thiazolyl, isoxazolyl, isothiazolyl, imidazolyl, tetrazolyl, pyrazolyl, pyrimidyl, pyrazinyl, quinolyl, isoquinolyl, benzofuryl, benzothienyl, benzimidazolyl, benzthiazolyl, benzoxazolyl, indolyl, isoindolyl, purinyl, or carbazolyl, wherein the substituent is independently selected from the group consisting of hydrogen, C1-6 alkyl, halogen, C3-6 cycloalkyl, C1-3 acylamino, C1-4 alkoxy, C1-5 alkoxycarbonyl, cyano, trifluoromethyl, trifluoromethoxy, hydroxy, amino, C1-4 alkylamino, di-C1-4 alkylamino, and C1-5 alkylcarbonyloxy; R1 is selected from the group consisting of hydrogen, halogen, C1-10 alkyl, C3-6 cycloalkyl, and C1-3 alkoxy; and R3 is C1-4 alkyl, phenyl-C1-3 alkyl, diphenylmethyl, or triphenylmethyl; comprising the step of treating an amine of structural formula (III): wherein R2 is C1-4 alkyl; with an amine of structural formula (IV): in the presence of phosgene or a phosgene equivalent and base to produce a compound of structural formula (VI): â€ƒfollowed by treatment with aqueous acid.