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Processes for preparing a crystalline form of N-(2-(4-(4- fluorobenzylcarbamoyl) -5-hydroxy-1-methyl-6-oxo-1, 6-dihydropyrimidin-2- yl)propan-2-yl) -5-methyl-1,3,4-oxadiazole-2- carboxamide potassium salt

IP.com Disclosure Number: IPCOM000209501D
Publication Date: 2011-Aug-08
Document File: 2 page(s) / 56K

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         Processes for preparing a crystalline form of N-(2-(4-(4- fluorobenzylcarbamoyl) -5-hydroxy-1-methyl-6-oxo-1, 6-dihydropyrimidin-2- yl)propan-2-yl) -5-methyl-1,3,4-oxadiazole-2- carboxamide potassium salt

    N-(2-(4-(4-fluorobenzylcarbamoyl) -5-hydroxy-1-methyl-6-oxo-1, 6- dihydropyrimidin-2-yl)propan-2-yl) -5-methyl-1,3,4-oxadiazole-2- carboxamide potassium salt, referred to as Compound I, has the following structure:

O

OK

F

N

   N N

O

  HN O

HN

N

O

Processes for preparing a crystalline form of Compound I are described herein. The crystalline form of Compound I is characterized by data selected from: an X-

ray powder diffraction (XRPD) pattern having peaks at 8.0, 11.9, 14.9, 18.2, 19.8, 24.9,


26.6, 27.7 and 28.9 degrees two theta ± 0.2 degrees two theta; an X-ray powder diffraction pattern substantially as depicted in Figure 1; and a combination thereof,

Figure 1: XRPD of Crystalline Form of Compound I

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  The process for preparing a crystalline form of Compound I may comprise exposing amorphous form of Compound I to water. The process can be done, for example, by slurrying a sample of amorphous form of Compound I in water, preferably, within

1


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concentration of about 0.1 g/mL to about 2 g/mL, or by exposing amorphous form of Compound I to a relative humidity of about 30 % to about 90 %.

EXAMPLES

PXRD method

    The X-ray powder diffraction was performed on a SCINTAG X-Ray powder diffractometer model X'TRA equipped with a solid-state detector. Copper radiation of


1.5418 Å was used to analyze the samples, which were in round aluminum sample holders with zero background...