Novel crystals and process of making 5-([[2-amino-3-(4-carbamoyl-2, 6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1H-imidazol-2-yl)-ethyl]-amino]-methyl)-2-methoxy- benzoic acid

Novel crystals and process of making 5-([[2-amino-3-(4-carbamoyl-2, 6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1H-imidazol-2-yl)-ethyl]-amino]-methyl)-2-methoxy- benzoic acid

  • CN 105,111,149 A
  • Filed: 07/07/2008
  • Published: 12/02/2015
  • Est. Priority Date: 07/09/2007
  • Status: Active Application
First Claim
Patent Images

1. prepare 5-({ [2-amino-3-(4-carbamyl-2 for one kind;

  • 6-Dimethvl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazoles-2-base)-ethyl]-amino }-methyl) method of zwitterionic alpha type crystal of-2-methoxy-benzoic acid, comprise the steps;

    By strong ionizable acid and 5-({ [2-t-butoxycarbonyl amino-3-(4-carbamyl-2,6-Dimethvl-phenyl)-propionyl]-[1-(4-phenyl-1H-imidazoles-2-base)-ethyl]-amino-methyl) mixing of-2-methoxy-benzoic acid, to prepare the salt of 5-({ [2-amino-3-(4-carbamyl-2,6-Dimethvl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazoles-2-base)-ethyl]-amino }-methyl)-2-methoxy-benzoic acid;

    Described 5-({ [2-amino-3-(4-carbamyl-2 is washed with mineral alkali;

    6-Dimethvl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazoles-2-base)-ethyl]-amino }-methyl) salt of-2-methoxy-benzoic acid;

    to obtain the zwitter-ion of 5-({ [2-amino-3-(4-carbamyl-2,6-Dimethvl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazoles-2-base)-ethyl]-amino }-methyl)-2-methoxy-benzoic acid;

    AndStore to form 5-({ [2-amino-3-(4-carbamyl-2 by under the relative humidity of described zwitter-ion between 0-40%;

    6-Dimethvl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazoles-2-base)-ethyl]-amino }-methyl) the zwitterionic alpha type crystal of-2-methoxy-benzoic acidWherein said crystal is characterized by the x-ray diffractogram of powder case at the powder x-ray diffraction peak with the bottom lines being substantially similar to Fig. 1.

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