Patent ID: 6579987
Filing Date: 2003-06-17
Classification: A61P,C07C,C07D

Abstract:
A method for preparing a compound of the formula H whereinAr1 and Ar2 are independently selected aryl groups, optionally substituted with up to five substituents independently selected from the group consisting of alkyl, alkoxy, cycloalkyl, cycloalkyloxy, heterocycloalkyl, heterocycloalkyloxy, alkanoyl, thioalkyl, aralkyl, aralkyloxy, aryloxyalkyl, aryloxyalkoxy, cycloalkyl-substituted alkyl, cycloalkyloxy-substituted alkyl, cycloalkyl-substituted alkoxy, cycloalkyloxy-substituted alkoxy, heterocycloalkyl-substituted alkyl, heterocycloalkyloxy-substituted alkyl, heterocycloalkyl-substituted alkoxy, heterocycloalkyloxy-substituted alkoxy, thioaryl, aralkylthio, thioaryl-alkyl, aralkylthioalkyl, halo, NO2, CF3, CN, OH, alkylenedioxy, SO2NRRâ€², NRRâ€², CO2R (where R and Râ€² are independently selected from the group consisting of H and alkyl), and a second aryl group, which may be substituted as above; the method comprising: (a) reducing an ester of the formula C â€ƒto give an alcohol; (b) brominating the alcohol of (a) to provide a bromide D (c) alkylating a sarcosine ester with the bromide D to give the sarcosine intermediate E (d) removing the trimethylsilyl group of sarcosine intermediate E to provide the intermediate F (e) coupling a compound of the formula Ar1-I with the intermediate F to give the diaryl compound G (f) deprotecting the diaryl compound G to give the compound of the formula H.