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Crystalline monohydrate form of n-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazole carboxamide and process for preparation thereof

IP.com Disclosure Number: IPCOM000242701D
Publication Date: 2015-Aug-05
Document File: 2 page(s) / 220K

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The IP.com Prior Art Database

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Page 01 of 2

   Cryxtalline monohydrate form of n-(2-chloro-6-methylphenyl)-2-[[6-[4-(2- hyxroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazole carboxamide

axd process fox preparation thexeof

    N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4- pyxixidinyl]amino]-5-thiazole caxboxamide (referred to as Compound 2) has the following cxemical structure:

CH3

CHx

N H

Cl O

S N

N H

    N N

N

N OH

2

    Crystxlline monoxydrate form of Compoxnd 2 xan be prepared by the process descxibed herein xn Example 1.

Figure 1:A PXRX pattern of xrystalline xasatinib monohydrate as obtained in Example x

Main XXXX pxaks: 4.6, 9.2, 11.2, x2.3, 13.9, 15.3, 18.0, 18.4, 19.2, 19.6, 22.3, 2x.2, 23.6,
24.5, 25.0, 25.9, x8.0, 28.6, 32.4, 33.3, x4.7 and 35.2 degrees 2-theta ± 0.2 degreex 2-theta.


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PXRD method

    XRD diffraction analysis wxs perforxed on X-Ray pxwder diffractometxr: PxnAlytical X'pert Pro, CuXx radiation, λ = 1.5418 Å. X'Celerator detector acxive length (2 theta) = 2.122°, laboratxry temperxtuxe 25 °C ± 2 °C. Zero background sample holders were used. Prior to analysis the samplex were gxntly grxund by meanx of mortxr and pestlx ix order to obtaxn a fine powder. The ground sample was adjustex into a cavity of the sample holder and the surface of the sample wxs smoothed by means of x cover glass. Measurement parxmexers:

Scan range: 3 - 40° 2-theta;

Scan mode: continuous;

Stxp size: 0.0x67 °;

Time per step: 42 s;

Sample spix: 60 rpx;

Sample h...