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Crystalline forms of 2-isopropoxy-5-methyl-4-(piperidin-4-yl)aniline dihydrochloride and 2,5-dichloro-N-(2-(isopropylsulfonyl)phenyl)pyrimidin-4-amine

IP.com Disclosure Number: IPCOM000239591D
Publication Date: 2014-Nov-18
Document File: 3 page(s) / 451K

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The IP.com Prior Art Database

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Crystalline forms of

2-isopropoxy-5-methyl-4-(piperidin-4-yl)aniline dihydrochloride and

2,5-dichloro-N-(2-(isopropylsulfonyl)phenyl)pyrimidin-4-amine

Disclosed hereinafter is a crystalline forms of 2-isopropoxy-5-methyl-4-(piperidin-4-yl)aniline dihydrochloride (referred herein as compound I) and (2,5-dichloro-N-(2- (isopropylsulfonyl)phenyl)pyrimidin-4-amine (referred herein as compound II). Compound I and Compound II may be intermediates in the synthesis of 5-Chloro-N2-(2-isopropoxy-5- methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine.

Figure 1: a powder XRPD pattern of crystalline compound I:

Intensity (counts)

5000

4000

3000

2000

1000

0

5

10

15

20

25

30

35

2Theta (°)

XRPD peaks: 13.7, 14.1, 17.0, 18.6, 19.0, 20.3, 23.1, 24.0 and 26.2 degrees two theta ± 0.2 degrees two theta.

Figure 2: FTIR spectrum of crystalline crystalline compound I:


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Figure 3: a powder XRPD pattern of crystalline compound II:

Intensity (counts)

90000

62500

40000

22500

10000

2500

0

5

10

15

20

25

30

35

2Theta (°)

XRPD peaks: 9.1, 11.4, 12.3, 18.1, 20.1, 22.6, 25.0 and 27.3 degrees two theta ± 0.2 degrees two theta.

Figure 4: FTIR spectrum of crystalline crystalline compound II:


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X-

Ray Power Diffraction:

PXRD method:

After being powdered using mortar and pestle, samples were applied directly on a silicon plate holder. The X-ray powder diffraction pattern was measured with a Philips X'Pert PRO X-ray powder diffractometer, e...