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Crystalline form of (S)-3-(4-phenoxyphenyl)-1-(piperidin-3-yl)-1H-pyrazolo[3,4- d]pyrimidin-4-amine Hydrochloride Disclosure Number: IPCOM000236135D
Publication Date: 2014-Apr-08
Document File: 2 page(s) / 23K

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Crystalline form of (S)-3-(4-phenoxyphenyl)-1-(piperidin-3-yl)-1H-pyrazolo[3,4-
d]pyrimidin-4-amine Hydrochloride

(S)-1-(3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin- 1-yl)prop-2-en-1-one, referred to as Compound I, has the following structure:

    Described herein below, is a crystalline form of (S)-3-(4-phenoxyphenyl)-1- (piperidin-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine hydrochloride, referred to as compound II, which is an intermediate in the preparation of compound I.Samples of Compound II were prepared by the process described in example 1, and were analyzed by X-ray powder diffraction ("XRPD") to provide a crystalline form. Figure 1 presents the XRPD of the obtained form.

Figure 1: XRPD of the crystalline form of Compound II

°2 theta


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    According to figure 1, the crystalline form of Compound II is characterized by XRPD peaks at: 4.2, 8.3, 9.0, 9.7, 10.4, 10.8, 11.3, 12.5, 15.3, 16.3, 17.7, 18.2, 18.9,
19.7, 20.8, 21.8, 22.7, 23.7, 24.3, 25.3, 25.7, 26.7, 27.0, 27.3, 28.4, 28.9 and 30.7 degrees 2-theta ± 0.2 degrees 2-theta.

XRPD method

    The analyses were performed on ARL (SCINTAG) powder X-Ray diffractometer model X'TRA equipped with a solid state detector. Copper radiation of
1.5418 Å was used. Scanning parameters: range: 2-40 degrees two-theta; scan mode: continuous scan; step size: 0.05°, and a rate of 3deg/min.

Example 1: Process for preparing (S)-3-(4-phenoxyphenyl)-1-(piperidin-3-yl)-1H-