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Method for controlling impurities in pipericide

A technology of piperbocilide and a control method, which is applied in the field of impurity control in breast cancer drug piperbacillide, can solve problems such as poor impurities and low product purity, and achieve the effects of excellent quality, high purity and simple control method.

Inactive Publication Date: 2021-07-13
JIANGXI GUOYAO PHARMA LLC +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] In the prior art, there are many synthetic methods for palbociclib, but the control of impurities in the process is poor, resulting in problems such as low product purity

Method used

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  • Method for controlling impurities in pipericide
  • Method for controlling impurities in pipericide
  • Method for controlling impurities in pipericide

Examples

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Effect test

Embodiment 1

[0073] In the present embodiment, the purity of each intermediate is controlled as follows:

[0074] The purity of intermediate I is as follows: the compound I content is 0.4%, the compound II content is 1.5%, the largest single unknown impurity content is 1.2%, and the total impurity content is 3.4%.

[0075] The purity of intermediate II is as follows: the content of intermediate I is 0.1%, the largest single unknown impurity content is 1.0%, and the total impurity content is 2.3%.

[0076] The purity of palbociclib salt is as follows: the content of impurity L contained is 0.1%, the content of impurity K shall not exceed 0.1%, the content of impurity M is 0.2%, the content of impurity N is 0.2%, the content of the largest single unknown impurity is 0.1%, and the content of total impurities is 0.8%. .

[0077] The content of the generated final product palbociclib and the content of impurities contained therein were detected, and the results are shown in Table 1.

Embodiment 2

[0079] In the present embodiment, the purity of each intermediate is controlled as follows:

[0080] The purity of intermediate I is as follows: the compound I content is 0.3%, the compound II content is 1.1%, the largest single unknown impurity content is 0.9%, and the total impurity content is 2.7%.

[0081] The purity of intermediate II is as follows: the content of intermediate I contained is 0.1%, the largest single unknown impurity content is 0.9%, and the total impurity content is 1.8%.

[0082] The purity of palbociclib salt is as follows: the content of impurity L is 0.1%, the content of impurity K is 0.1%, the content of impurity M is 0.1%, the content of impurity N is 0.2%, the content of the largest single unknown impurity is 0.1%, and the content of total impurities is 0.7%.

[0083] The content of the generated final product palbociclib and the content of impurities contained therein were detected, and the results are shown in Table 1.

Embodiment 3

[0085] In the present embodiment, the purity of each intermediate is controlled as follows:

[0086] The purity of intermediate I is as follows: the compound I content is 0.3%, the compound II content is 1.4%, the largest single unknown impurity content is 1.1%, and the total impurity content is 3.5%.

[0087] The purity of intermediate II is as follows: the content of intermediate I is 0.2%, the largest single unknown impurity content is 0.9%, and the total impurity content is 3.0%.

[0088] The purity of the palbociclib salt is as follows: the impurity L content is 0.1%, and the impurity K content is 0.1%. The impurity M content is 0.1%, the impurity N content is 0.2%, the largest single unknown impurity content is 0.2%, and the total impurity content is 0.9%.

[0089] The content of the generated final product palbociclib and the content of impurities contained therein were detected, and the results are shown in Table 1.

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Abstract

The invention discloses a method for controlling impurities in pipericide, and relates to the technical field of pharmaceutical chemical. The content of the impurities in the pipericide is reduced by controlling the purity of an obtained intermediate I. The content of a compound I in the intermediate I does not exceed 1.0%, the content of a compound II in the intermediate I does not exceed 5.0%, the content of a compound III in the intermediate I does not exceed 5.0%, the maximum single unknown impurity content does not exceed 2.0%, and the total impurity content does not exceed 9.0%. The method has the beneficial effect that main organic impurities can be effectively controlled by controlling the purity of the intermediate. The control method disclosed by the invention is simple and easy to realize, the product with higher purity and better quality is obtained, and the method is suitable for being applied to industrial production.

Description

technical field [0001] The invention relates to the technical field of medicine and chemical engineering, in particular to a method for controlling impurities in the breast cancer drug palbociclib. Background technique [0002] Palbociclib is a targeted CDK4 / 6 inhibitor, which was first reported by US Patent 6936612. Its chemical name is: 6-acetyl-8-cyclopentyl-5-methyl-2-[[5-(1-piperazinyl)-2-pyridyl]amino]pyridine[2,3-d] Pyrimidin-7(8H)-one, chemical structure: [0003] [0004] Molecular formula: C24H29N7O2 [0005] Molecular weight: 447.53 [0006] Palbociclib selectively inhibits cyclin-dependent kinases 4 and 6 (CDK4 / 6), restores cell cycle control, and blocks tumor cell proliferation. Palbociclib combined with letrozole for postmenopausal women with estrogen receptor-positive (ER+), human epidermal growth factor receptor 2-negative (HER2-) advanced or metastatic breast cancer who have not previously received systemic therapy to control advanced disease The ini...

Claims

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Application Information

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IPC IPC(8): C07D471/04
CPCC07D471/04
Inventor 彭彪杨明孟周钧
Owner JIANGXI GUOYAO PHARMA LLC
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