Patent ID: 7223870
Filing Date: 2007-05-29
Classification: A61P,C07D

Abstract:
1. A method for preparing a compound of formula I wherein R R phenyl optionally substituted with C or benzyl with the phenyl moiety of the benzyl optionally substituted with C 1 –C 6 alkoxy or OY wherein Y is a hydroxy protecting group, halogen, C 1 –C 4 alkyl, C 2 –C 6 alkenyl, C 2 –C 6 alkynyl, C 1 –C 4 alkoxy-C 1 –C 4 alkyl, trifluoromethyl, amido, nirto, carbo-C 1 –C 4 alkoxy, C 1 -C 4 alkoxy-carbonyl, carbonyl or cyano; wherein is Ar is an aromatic hydrocarbon or heteroaromatic moiety selected from the group consisting of phenyl, naphthyl, pyridyl, thiophenyl, furanyl, pyrrolyl and pyrimidyl, imidazolyl, oxazolyl, thiazolyl, triazolyl, pyrazolyl, pyrazinyl, pyridazinyl each of which may be optionally substituted by one or more, preferably one to two, substituents independently selected from the group consisting of halogen, hydroxyl, C comprising reacting a compound of formula II wherein R R phenyl optionally substituted with C or benzyl with the phenyl moiety of the benzyl optionally substituted with C 1 –C 6 alkoxy or OY wherein Y is a hydroxy protecting group, halogen, C 1 –C 4 alkyl, C 2 –C 6 alkenyl, C 2 –C 6 alkynyl, C 1 –C 4 alkoxy-C 1 –C 4 alkyl, trifluoromethyl, amido, nirto, carbo-C 1 –C 4 alkoxy, C 1 –C 4 alkoxy-carbonyl, carbonyl or cyano; with an aryl halide of formula III wherein Ar is an aromatic hydrocarbon or heteroaromatic moiety selected from the group consisting of phenyl, naphthyl, pyridyl, thiophenyl, furanyl, pyrrolyl and pyrimidyl, imidazolyl, oxazolyl, thiazolyl, triazolyl, pyrazolyl, pyrazinyl, and pyridazinyl each of which may be optionally substituted by one or more, preferably one to two, substituents independently selected from the group consisting of halogen, C L is an activated leaving group, such as a halide, preferably iodide or bromide; or alkyl- or aryl-sulfonate, such as mesylate, triflate, tosylate in the presence of N,N-dimethyl ethylenediamine and in the presence of a copper catalyst.