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Crystalline form of (R)-5-(2-fluoro-3-methoxyphenyl)-1-(2-fluoro-6-(trifluoromethyl) benzyl)-6-methyl-3-(2-phenyl-2-(propan-2-ylideneamino)ethyl)pyrimidine-2,4(1H,3H)- dione

IP.com Disclosure Number: IPCOM000246953D
Publication Date: 2016-Jul-18
Document File: 3 page(s) / 343K

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The IP.com Prior Art Database

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Crystalline form of (R)-5-(2-fluoro-3-methoxyphenyl)-1-(2-fluoro-6-(trifluoromethyl) benzyl)-6-methyl-3-(2-phenyl-2-(propan-2-ylideneamino)ethyl)pyrimidine-2,4(1H,3H)- dione

Disclosed herein after is a process for preparation of (R)-5-(2-fluoro-3-methoxyphenyl)-1-(2- fluoro-6-(trifluoromethyl) benzyl)-6-methyl-3-(2-phenyl-2-(propan-2- ylideneamino)ethyl)pyrimidine-2,4(1H,3H)-dione (referred herein as compound I) and crystalline form thereof.

Compound I and crystalline form thereof may be used in the preparation of (R)-4-[[2-[5-(2- fluoro-3-methoxyphenyl)-3-[[2-fluoro-6-(trifluoromethyl)phenyl]methyl]-4-methyl-2,6- dioxo-3,6-dihydropyrimidin-1(2H)-yl]-1-phenylethyl]amino]butanoic acid. This process may provide easier handling and purification.

Crystalline form I of compound I

The crystalline form I of comound I may be characterized by an X-ray powder diffraction pattern having peaks at: 4.56, 9.08, 9.78, 10.54, 11.71, 12.17, 13.19, 14.79, 16.03, 16.64,
17.36, 18.20, 18.60, 19.21, 20.14, 22.23, 22.67, 23.25, 24.06, 24.73, 25.04, 26.46, and 27.42 ± 0.2 °2θ; and/or an X-ray powder diffraction pattern as depicted in Figure 1; and/or an FTIR spectrum as depicted in Figure 2.

6000

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0

Figure 1. XRPD of crystalline form I of compound I

Intensity (counts)

5

10 15 20 25 30 35

2Theta (°)


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%T

40

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20

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1000

Wavenumbers (cm-1)

Figure 2. FTIR spectrum of crystalline form I of compound I

XRPD method:

After being powdered using mortar and pestle, samples were applied directly on a silicon plate holder. The X-ray powde...