| 摘要 |
600273 Disclosed is a process for the preparation of Aleglitazar ((S)-2-methoxy-3-{ 4-[2-(5-methyl-2-phenyl-oxazol-4-yl)-ethoxy]benzo[b]thiophen-7-yl} -propionic acid) as represented by formula (I), or a salt thereof, wherein a compound of formula (II) or a salt thereof is hydrogenated in the presence of a catalyst comprising iridium and a compound of formula (X) wherein R1 is hydrogen, alkyl, aryl or arylalkyl; and R2 is aryl, and particularly where the catalyst is [Ir((Sa,R)-7-[4,5-dihydro-4-benzyloxazol-2-yl]-7’-di(3,5-di-tert-butylphenyl)phosphino-1,1’-spirobiindane)(1,5-cyclooctadiene)][tetrakis[3,5-bis(trifluoromethyl)phenyl]borate], [Ir((Sa,R)-7-[4,5-dihydro-4-benzyloxazol-2-yl]-7’-di(3,5-di-tert-butylphenyl)phosphino-1,1’-spirobiindane)(1,5-cyclooctadiene)][tetrafluoroborate], [Ir((Sa,R)-7-[4,5-dihydro-4-benzyloxazol-2-yl]-7’-di(3,5-di-tert-butylphenyl)phosphino-1,1’-spirobiindane)(1,5-cyclooctadiene)][trifluoromethanesulfonate] or [Ir((Sa,R)-7-[4,5-dihydro-4-benzyloxazol-2-yl]-7’-di(3,5-di-tert-butylphenyl)phosphino-1,1’-spirobiindane)(1,5-cyclooctadiene)][chloride]. . |
