Patent ID: 6384223
Filing Date: 2002-05-07
Classification: C07D

Abstract:
A process for preparing a compound of formula 1: wherein:X is phenyl optionally substituted with one or more substituents selected from the group consisting of halogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, hydroxy, trifluoromethyl, cyano, nitro, carboxy, carboalkoxy of 2-7 carbon atoms, carboalkyl of 2-7 carbon atoms, amino, and alkanoylamino of 1-6 carbon atoms; R and R1 are each, independently, hydrogen, halogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, hydroxy, or trifluoromethyl; R2 is hydrogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, hydroxy, trifluoromethyl; R3 is independently hydrogen, alkyl of 1-6 carbon atoms, carboxy, carboalkoxy of 1-6 carbon atoms, phenyl, or carboalkyl of 2-7 carbon atoms; n=2-4; or a pharmaceutically acceptable salt thereof, with the proviso that each R3 of Y may be the same or different, which comprises:a) acylating a compound of the formula: â€ƒwith an acid chloride or mixed anhydride having the formula: â€ƒwherein Z is â€”OR4, â€”SR4, â€”SOR4, â€”SO2R4, halogen, â€”NHR5, or â€”NR5R5; R4 is alkyl of 1-6 carbon atoms, cycloalkyl of 3-8 carbon atoms, or phenyl; R5 is alkyl of 1-6 carbon atoms or cycloalkyl of 3-8 carbon atoms; L is Cl, Br, or â€”OC(O)R6; R6 is alkyl of 1-6 carbon atoms, cycloalkyl of 3-8 carbon atoms, or phenyl; R3 and n are as defined above; b) reacting the acylated product of step a) with H2Nâ€”X, â€ƒwherein X is as defined above; and c) treating the compound of step b) with a mild base to give the compound of Formula 1.