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Deuterated Palbociclib crystal

A technology of crystallization and deuteration, applied in the directions of organic chemistry, organic chemistry method, drug combination, etc., can solve problems such as unreported crystallization, and achieve the effects of simple preparation method, mild crystallization conditions and high purity

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 has not been reported

Method used

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  • Deuterated Palbociclib crystal
  • Deuterated Palbociclib crystal
  • Deuterated Palbociclib crystal

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0039]

[0040] Add the compound of formula I (607 mg, 1 mmol) into a 50 mL three-neck flask containing 14.4 mL of anisole and 9.6 mL of n-butanol in an oil bath and heat to 100°C to condense and reflux. After the reaction dissolves, turn off heating and stirring, and transfer the reaction after cooling to room temperature Put it in the refrigerator at 4°C overnight and then filter it with suction. The filter cake is washed with anisole and then with n-heptane, and the obtained solid is dried in a vacuum oven at 50°C. The pale yellow compound (468 mg, 0.77 mmol) was obtained with a yield of 77%.

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Abstract

The invention provides a deuterated Palbociclib crystal shown in the formula I and a preparation method and pharmaceutical application thereof and particularly relates to a deuterated Palbociclib crystal shown in the formula I, a preparation method of the crystal, a crystal composition containing the crystal, a pharmaceutical composition containing the crystal and the crystal composition thereof and pharmaceutical application of the crystal and the crystal composition thereof. The crystal has the advantages of being high in purity and crystallinity, good in stability and easy to prepare, and can be used for preparing medicine for treating diseases caused by cyclin dependent kinase 4 and 6. The formula I is shown in the specification.

Description

technical field [0001] The present invention relates to the crystallization of pharmaceutical compounds, in particular, the present invention relates to a deuterated palbociclib crystallization. The present invention also relates to a preparation method of the deuterated Palbociclib crystal, a crystal composition containing the deuterated Palbociclib crystal, a pharmaceutical composition and its application 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 phosphorylation of different substrate...

Claims

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Application Information

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IPC IPC(8): C07D471/04A61P35/00
CPCC07D471/04C07B2200/13
Inventor 张寅生高勇王昭
Owner CHIA TAI TIANQING PHARMA GRP CO LTD
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