Resolution of (±)-methyl...

Details Resolution of (±)-methyl... Resolution of (±)-methyl...

C - Chemistry, Metallurgy

07

D

C07D 211/34 (2006.01) A61K 31/451 (2006.01)

Patent

CA 2757702

The present invention relates to a resolution process of (~)-methyl phenyl[4- [4-[[[4'-(trifluoromethyl)-2-biphenylyl] carbonyl]amino]phenyl]-1-piperidinyl]acetate to isolate the MTP (microsomaltriglyceride transfer protein) inhibitor methyl (2S)-phenyl[4-[4-[[[4'-(trifluoromethyl)-2-biphenylyl]carbonyl]amino]phenyl]-1- piperidinyl]-acetate and an epimerisation procedure for racemizing methyl (2R)-phenyl[4-[4-[[[4'-(trifluoromethyl)-2- biphenylyl]carbonyl]amino]phenyl]-1-piperidinyl]acetate.

La présente invention porte sur un procédé de résolution de (±)-phényl[4-[4-[[[4'-(trifluorométhyl)-2-biphénylyl]carbonyl]amino]phényl]-1-pipéridinyl]acétate de méthyle pour isoler l'inhibiteur de MTP (protéine microsomique de transfert de triglycérides) (2S)-phényl[4-[4-[[[4'-(trifluorométhyl)-2-biphénylyl]carbonyl]amino]phényl]-1-pipéridinyl]acétate de méthyle et sur un mode opératoire d'épimérisation pour la racémisation de (2R)-phényl[4-[4-[[[4'-(trifluorométhyl)-2-biphénylyl]carbonyl]amino]phényl]-1-pipéridinyl]acétate de méthyle.

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