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Crystalline form of (S)-N4-(3-chloro-4-fluorophenyl)-7-(tetrahydrofuran-3-yloxy)quinazoline-4,6-diamine

IP.com Disclosure Number: IPCOM000239237D
Publication Date: 2014-Oct-23
Document File: 3 page(s) / 189K

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                  Crystalline form of
(S)-N4-(3-chloro-4-fluorophenyl)-7-(tetrahydrofuran-3-yloxy)quinazoline-4,6-diamine

(S)-N4-(3-chloro-4-fluorophenyl)-7-(tetrahydrofuran-3-yloxy)quinazoline-4,6-diamine (previously referred in IPCOM000234585D as compound A-8) may be an intermediate in the synthesis of N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6- quinazolinyl]-4(dimethylamino)-2-butenamide. Disclosed herein after is acrystalline Form VII of compound A-8.

Crystalline Form VII of Compound A-8

The crystalline form VII of Compound A-8 is characterized by an X-ray powder diffraction pattern having peaks at: 5.9, 13.1, 15.2, 17.8, 19.3, 20.4, 21.5, 24.6 and 25.1 degrees two theta ± 0.2 degrees two theta; and/or an X-ray powder diffraction pattern as depicted in Figure 1; and/or an FTIR spectrum as depicted in Figure 2.

Intensity (counts)

5000

4000

3000

2000

1000

0

5

10

15

20

25

30

35

2Theta (°)

Figure 1. PXRD pattern of crystalline (S)-N4-(3-chloro-4-fluorophenyl)-7-(tetrahydrofuran-3- yloxy)quinazoline-4,6-diamine form VII in mixture with form VI.


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Figure 2. FTIR spectrum of crystalline (S)-N4-(3-chloro-4-fluorophenyl)-7-(tetrahydrofuran-3- yloxy)quinazoline-4,6-diamine form VII in mixture with form VI.

Experimental:

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, equipped with a Cu irradiation source = 1.54184 Ǻ (Ǻngström), X'Celerator...