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Crystalline forms of 4-(4-Fluoro-benzyl)-2-nitro-benzene-1,4-diamine

IP.com Disclosure Number: IPCOM000215229D
Publication Date: 2012-Feb-22
Document File: 2 page(s) / 71K

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Crystalline forms of 4-(4-Fluoro-benzyl)-2-nitro-benzene-1,4-diamine

    N-(2-Amino-4-(4-fluorobenzylamino)-phenyl-) carbamic acid ethyl ester referred to as Compound I, has the following formula:

                     Compound I 4-(4-Fluoro-benzyl)-2-nitro-benzene-1,4-diamine, referred to as Compound II, is an intermediate in the synthesis of Compound I.

Crystalline forms A and B of Compound II, are described herein.

Crystalline form A of Compound II is characterized by data selected from: an X-

ray powder diffraction (XRPD) pattern having peaks at 8.0, 11.6, 11.9, 13.0, 13.7,


14.1, 14.4, 15.1, 15.9, 16.8, 18.1, 19.5, 21.3, 21.7, 22.0, 22.5, 23.1, 23.6, 23.9, 24.6,


25.0, 25.3, 25.8, 26.9, 27.3, 27.6, 28.0, 29.1, 29.5, 29.9 and 30.8 degrees two-theta ±


0.2 degrees two-theta; an XRPD pattern as depicted in Figure 1; and a combination thereof.

   Crystalline form B of Compound II is characterized by data selected from: an XRPD pattern having peaks at 8.0, 9.2, 11.3, 11.5, 12.7, 13.2, 14.0, 14.2, 15.3, 16.1,


17.1, 17.4, 18.4, 20.0, 20.3, 22.0, 22.4, 23.2, 23.5, 24.2, 25.2, 25.6, 26.5, 26.9, 27.7,


28.1, 28.5, 29.0, 29.3, 29.6 and 30.8 degrees two-theta ± 0.2 degrees two-theta; an XRPD pattern as depicted in Figure 2; and a combination thereof.

Figure 1: XRPD of crystalline form A of Compound II.

8000

6000

4000

2000

0


2.0 6.0 10.0 14.0 18.0 22.0 26.0 30.0 34.0 38.0


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Figure 2: XRPD of crystalline form B of Compound II.

12000

8000

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0


6.0 10.0 14.0 18.0 22.0 26.0 30.0 34.0 38.0

XR...