PROCESS TO CHIRAL BETA AMINO ACID DERIVATIVES BY ASYMMETRIC HYDROGENATION
摘要
The present invention relates to a process for the efficient preparation of enantiomerically enriched beta amino acid derivatives which are useful in the asymmetric synthesis of biologically active molecules. The process comprises an enantioselective hydrogenation of a prochiral beta amino acrylic acid derivative substrate in the presence of a transition metal precursor complexed with a chiral ferrocenyl diphosphine ligand with in situ protection of the primary amine product. The invention also relates to a novel process for the preparation of chiral beta-amino acid amides as inhibitors of the dipeptidyl peptidase-IV of structural formula III and the useful intermediates obtained therein. The products resulting from the instant process are inhibitors of dipeptidyl peptidase-IV and thereby useful for the treatment of Type 2 diabetes.
申请公布号
WO2006065826(A2)
申请公布日期
2006.06.22
申请号
WO2005US45096
申请日期
2005.12.12
申请人
MERCK & CO., INC.;BIFTU, TESFAYE;SONG, ZHIGUO, J.;ZHANG, FEI;ROSNER, THORSTEN;HANSEN, KARL;ARMSTRONG, JOSEPH, D., III
发明人
BIFTU, TESFAYE;SONG, ZHIGUO, J.;ZHANG, FEI;ROSNER, THORSTEN;HANSEN, KARL;ARMSTRONG, JOSEPH, D., III