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Crystalline form of (S)-N-(3-chloro-4-fluorophenyl)-6-nitro-7-(tetrahydrofuran-3-yloxy)quinazolin-4-amine

IP.com Disclosure Number: IPCOM000240504D
Publication Date: 2015-Feb-04
Document File: 3 page(s) / 213K

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                     Crystalline form of
(S)-N-(3-chloro-4-fluorophenyl)-6-nitro-7-(tetrahydrofuran-3-yloxy)quinazolin-4-amine


(S)-N-(3-chloro-4-fluorophenyl)-6-nitro-7-(tetrahydrofuran-3-yloxy)quinazolin-4-amine (previously referred in IPCOM000234585D as compound A-7) 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 II of compound A-7.

Crystalline Form II of Compound A-7

The crystalline form II of Compound A-7 is characterized by an X-ray powder diffraction pattern having peaks at: 7.6, 10.2, 11.1, 12.2, 17.5, 17.8, 21.2, 26.0, 26.6, 27.1 ± 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)

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2Theta (°)

Figure 1. PXRD pattern of crystalline (S)-N-(3-chloro-4-fluorophenyl)-6-nitro-7- (tetrahydrofuran-3-yloxy)quinazolin-4-amine crystalline form II.


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Figure 2. FTIR spectrum of crystalline (S)-N-(3-chloro-4-fluorophenyl)-6-nitro-7- (tetrahydrofuran-3-yloxy)quinazolin-4-amine crystalline form II.

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...