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Amorphous 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

IP.com Disclosure Number: IPCOM000203870D
Publication Date: 2011-Feb-07
Document File: 2 page(s) / 26K

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 Amorphous 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
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 is known as RLT free hydroxy. RLT free hydroxy of the following chemical structure:

O

OH

F

N

N

N

H

N

H

N

O

N

O

O

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   Amorphous form of RLT free hydroxy was found and described herein. Amorphous form of RLT free hydroxy is characterized by an XRPD pattern as depicted in figure 1.

Figure 1: XRPD of Amorphous form of RLT free hydroxy

Counts

2000

1000

0

5 10 15 20 25

Position [°2Theta] (Copper (Cu))

Examples:

PXRD


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Powder X-ray diffraction data were obtained by using conventional methods employing a SCINTAG powder X-Ray 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. Scanning parameters: Range: 2-40 deg. 2 theta. All peak positions reported are within ±0.2 degrees two theta.

Example 1: Preparation of Amorphous form of RLT free hydroxy

A flask (100 ml) was charged with RLT-Free (4 g) and Acetone (60 ml). The mixture was heated to 35-45oC until dissolution. The solution was filtered and sprayed.

The nitrogen gas was at an inlet temperature of 60-70°C. The evapora...