Patent ID: 7067671

Claim:
A process for preparing a compound of formula (I) wherein R 1 is selected from the group consisting of phenyl, substituted phenyl, (where the substituents are selected from C 1 –C 5 alkyl, halogen or trifluoromethyl); R 2 is a saturated or unsaturated 6 membered ring with 5 carbon atoms and one nitrogen atom; R 3 is carbocyclic arylC 1 –C 5 alkyl, wherein the aryl group is optionally substituted with substituents selected from C 1 –C 5 alkyl, C 1 –C 5 alkoxy, halogen, amino, C 1 –C 5 alkylamino or di(C 1 –C 5 alkyl) amino); R 4 is where p is an integer from 0 to 9; X is selected from the group consisting of hydrogen, hydroxy, vinyl, substituted vinyl, (where one or more substituents are selected from fluorine or chlorine), ethynyl, substituted ethynyl (where the substituent is selected from fluorine or chlorine), C 1 –C 5 alkyl, substituted C 1 –C 5 alkyl (where the alkyl substituents are selected from one or more of C 1 –C 5 alkoxy and trihaloalkyl,), and C 3 –C 7 cycloalkyl and pharmaceutically acceptable salts thereof; comprising reacting a compound of formula (VIII), wherein L 1 and L 2 are independently selected from the group consisting of C 1 –C 4 alkyl and C 1 –C 4 aralkyl; or L 1 together with L 2 is selected from the group consisting of —CH 2 —CH 2 —(optionally substituted with one to four C 1 –C 3 alkyl), and —CH 2 —CH 2 —CH 2 —(optionally substituted with one to six C 1 –C 3 alkyl); with a compound of formula (X), to produce the corresponding compound of formula (XI); cyclizing the compound of formula (XI), under acid conditions of pH less than about 7, to produce the corresponding compound of formula (XII); reacting the compound of formula (XII) with POBr 3 , PBr 5 , or a mixture of PBr 3 and Br 2 , to yield the corresponding compound of formula (XIII); displacing the bromine on the compound of formula (XIII) by reacting with a compound of formula (XIV), to produce the corresponding compound of formula (I).