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New crystal form substance of Dasatinib anhydrous substance and preparation method thereof

A technology of dasatinib and hydrate, which is applied in the field of new crystal form of dasatinib anhydrate and its preparation, can solve the problem of inability to reduce the product, and achieve industrialization and high reaction selectivity , quality controllable effect

Inactive Publication Date: 2016-04-20
HARBIN PHARMA GROUP TECH CENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0015] There are still certain shortcomings in the existing technology, that is, it is impossible to effectively reduce the related substances of the product in the preparation process to improve product quality

Method used

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  • New crystal form substance of Dasatinib anhydrous substance and preparation method thereof
  • New crystal form substance of Dasatinib anhydrous substance and preparation method thereof
  • New crystal form substance of Dasatinib anhydrous substance and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Add 12kg of crude dasatinib and 360L of anhydrous methanol into the reactor, stir and heat at room temperature to 65°C, grow crystals for 1 hour, and cool down to room temperature naturally. Suction filtration, washing the filter cake with anhydrous methanol and suction drying, and drying under reduced pressure at 45-55°C and vacuum degree ≤-0.090MPa. Obtained 8.9kg of white new crystalline form of dasatinib anhydrate, with a yield of 74.2% and a product purity of 99.94%.

Embodiment 2

[0056] Add 12kg of crude dasatinib and 240L of anhydrous methanol into the reactor, stir and heat to 40°C, grow crystals for 10 minutes, and cool down to room temperature naturally. Suction filtration, washing the filter cake with anhydrous methanol and suction drying, and drying under reduced pressure at 45-55°C and vacuum degree ≤-0.090MPa. Obtained 7.1 kg of white new crystal form of dasatinib anhydrate, with a yield of 59.2% and a product purity of 99.80%.

Embodiment 3

[0058] Add 12kg of crude dasatinib and 1200L of anhydrous methanol into the reactor, stir and heat at room temperature 25°C, grow crystals for 0.5 hours after complete dissolution, and then cool down to room temperature naturally. Suction filtration, washing the filter cake with anhydrous methanol and suction drying, and drying under reduced pressure at 45-55°C and vacuum degree ≤-0.090MPa. Obtained 8.4kg of white new crystal form of dasatinib anhydrate, with a yield of 70.0% and a product purity of 99.62%.

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Abstract

The invention discloses a new crystal form substance of a Dasatinib anhydrous substance and a preparation method thereof, belonging to the technical field of medicines. An X-ray powder diffraction pattern of the new crystal form substance has characteristic peaks at the following diffraction angles 2theta: 6.400+ / -0.2 degrees, 7.067+ / -0.2 degrees, 12.562+ / -0.2 degrees, 13.372+ / -0.2 degrees, 13.942+ / -0.2 degrees, 16.939+ / -0.2 degrees, 17.406+ / -0.2 degrees, 18.709+ / -0.2 degrees, 19.376+ / -0.2 degrees, 21.206+ / -0.2 degrees, 22.229+ / -0.2 degrees, 24.562+ / -0.2 degrees, 25.036+ / -0.2 degrees and 27.912+ / -0.2 degrees. The Dasatinib new crystal form substance prepared by the method has the advantages of high purity, stability, suitability for large-scale industrial production, and the like.

Description

technical field [0001] The invention relates to a new crystal form of dasatinib anhydrate and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Dasatinib chemical name: N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl Base-4-pyrimidinyl]amino]-1,3-thiazole-5-amide [0003] The structural formula is: [0004] [0005] Molecular formula: C 22 h 26 ClN 7 o 2 S [0006] Molecular weight: 488.01 [0007] Dasatinib, trade name Sprycel, previously known as BMS-354825, is a tyrosine kinase inhibitor produced by Bristol-Myers Squibb, which is mainly used for chronic granulocytes in the late stage of imatinib treatment Chronic myelogenous leukemia (chronicmyelogenousleukemia) and Philadelphia chromosome positive acute myeloid leukemia (Ph+ALL) patients. The drug has also been shown to treat many other types of cancer, including accelerated-stage prostate cancer. Dasatinib mainly targets P...

Claims

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Application Information

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IPC IPC(8): C07D417/12
CPCC07D417/12C07B2200/13
Inventor 袁淑杰杨新春王立东孙磊于海涛魏涛曹翊婕户巧芬黄炎曲学伟刘勇李郑武高晶赵华南关录凡
Owner HARBIN PHARMA GROUP TECH CENT
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