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Crystallization of deuteration Palbociclib isethionate

A technology of isethionate and crystallization, applied in the field of crystallization of pharmaceutical compounds, and can solve problems such as unreported crystallization

Inactive Publication Date: 2017-02-22
CHIA TAI TIANQING PHARMA GRP CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the prior art, WO2014150925 and CN104447739A disclose a variety of deuterated Palbociclib compounds, but the crystallization of deuterated Palbociclib isethionate has not been reported

Method used

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  • Crystallization of deuteration Palbociclib isethionate
  • Crystallization of deuteration Palbociclib isethionate
  • Crystallization of deuteration Palbociclib isethionate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0046]

[0047] Add compound II (0.5 g, 1.11 mmol) and methanol (2 mL) to the reaction flask respectively, and stir at room temperature to form a suspension. Isethionic acid (0.14 g, 1.11 mmol) was added dropwise to the suspension. The solid dissolved rapidly and then precipitated a yellow solid. Methanol (2 mL) was added, and the temperature was raised to 45° C. and stirred for 4 hours. Slowly let cool to room temperature, and cooled and precipitated at 4°C overnight. A yellow solid was obtained by suction filtration, and dried in a vacuum oven at 50°C to obtain deuterated palbociclib isethionate crystals (0.55 g) as shown in Formula I.

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Abstract

The invention provides a crystallization, preparation method and medical application of a deuteration Palbociclib isethionate as shown in the formula I and particularly relates to the crystallization of the deuteration Palbociclib isethionate shown in equation I, a preparation method of the crystal, the crystal compositions containing the crystal, the medicine compositions containing the crystal and the crystal compositions, and the medical application of the crystal and the crystal compositions. The crystal has the advantages of having high purity and high crystallinity, having good stability and being easy to prepare. The crystal can be adopted for the preparation of drugs for the treatment of the diseases caused by cyclin dependent kinase 4 and 6. Please see the formula in the description.

Description

technical field [0001] The present invention relates to the crystallization of pharmaceutical compounds, in particular, the present invention relates to a crystallization of deuterated palbociclib isethionate. The present invention also relates to a method for preparing crystals of deuterated Palbociclib isethionate, a crystal composition containing crystals of deuterated Palbociclib isethionate, a pharmaceutical composition and its use in the field of medicine. Background technique [0002] Cyclin-dependent protein kinases (CDKs) are important cellular enzymes that play important functions in regulating cell differentiation and proliferation. Cyclin-dependent kinases are a group of serine / threonine protein kinases that cooperate with cyclin and are important factors in cell cycle regulation. CDK can combine with cyclin to form a heterodimer, in which CDK is the catalytic subunit, and cyclin is the regulatory subunit. Different cyclin-CDK complexes can regulate the phosphor...

Claims

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Application Information

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IPC IPC(8): C07D471/04A61K31/519A61P35/00
CPCC07D471/04C07B59/002C07B2200/05C07B2200/13
Inventor 张寅生高勇
Owner CHIA TAI TIANQING PHARMA GRP CO LTD
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