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A process 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 sodium

IP.com Disclosure Number: IPCOM000237096D
Publication Date: 2014-Jun-01
Document File: 2 page(s) / 31K

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   A process 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 sodium

   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 sodium salt, referred herein as Compound I, has the following chemical structure:

   Provided herein is a process for preparing a crystalline form of Compound I. The process is described in Example 1. The isolated samples were analyzed by X-ray powder diffraction ("XRPD"), which indicated a formation of a crystalline form of Compound I. Figure 1 depicts the XRPD of the obtained crystalline form.

Figure 1: XRPD of a crystalline form of Compound I

Degrees two-theta



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    According to Figure 1, the crystalline form of Compound I is characterized by XRPD peaks at:7.6, 7.8, 11.3, 11.8, 13.3, 17.3, 19.6, 23.7, 26.3 and 28.0± 0.2 degrees two theta ± 0.2 degrees two theta.

XRPD method: Instrument: Thermo ARL, Scintag X-Ray powder diffractometer model X'TRA, Cu-tube, solid state detector or equivalent.
2-40 degrees two-theta range of measurement using scan mode, continuous scan, step size: 0.05 deg. and Scan rate: 3 deg./min.

Example 1: A process for preparing a crystalline form of Compound I

    A solution of NaOH (4.2 g) in /W Water (2 V) was added to N-(2-(4-(4- fluorobenzylcarbamoyl) -5-hydroxy-1-methyl-6-oxo-1, 6-dihydropyrimidin-2...