Preparation method for palbociclib

A preparation step, acetyl group technology, applied in the field of preparation of the drug palbociclib, can solve the problems of complex synthesis, rare, complex side reactions, etc., and achieve the effect of economical and environmental protection, simple process, and easy-to-obtain raw materials
CN104447743AActive Publication Date: 2015-03-25铜陵王燕堂生物科技有限公司
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
铜陵王燕堂生物科技有限公司
Publication Date
2015-03-25

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Abstract

The invention discloses a preparation method for palbociclib (I). The preparation method comprises the following steps: performing cyclization reaction on 2-acetyl-2-butenoic acid methyl ester and malononitrile under an alkaline condition to generate 1,4,5,6-4H-2-methoxyl-4-methyl-5-acetyl-6-oxo-3-pyridine carbonitrile (II); performing substitution reaction on the intermediate (II) and cyclopentane halide (III) under the action of an acid-binding agent to generate N-cyclopentyl-1,4,5,6-4H-2-methoxyl-4-methyl-5-acetyl-6-oxo-3-pyridine carbonitrile (IV); performing condensation reaction on the intermediate (IV) and N-[5-(1-piperazinyl)-2-piperidyl]carbamidine (V)to generate 6-acetyl-8-cyclopentyl-5-methyl-2-[[5-(1-piperazinyl)-2-pyridyl]amino]-5,6-dihydropyrido[2,3-d]pyrimidine-7(8H)-ketone (VI); performing dehydrogenation reaction on the intermediate (VI) and sodium selenate to generate the palbociclib (I). The preparation method for the palbociclib has the advantages that the raw material is easy to obtain, the process is simple, high efficiency and environmental protection are achieved, and the preparation method is suitable for industrial production.
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Description

technical field

[0001] The invention belongs to the technical field of organic synthesis route design and preparation of raw materials and intermediates, and in particular relates to a preparation method of palbociclib, which may be used to treat breast cancer. Background technique

[0002] Palbociclib (Palbociclib) is a cell cycle-dependent kinase (CDK4 / 6) inhibitor developed by Pfizer, which was granted the "Breakthrough Therapy" qualification by the US FDA in April 2013. Due to its good clinical performance in Phase III, Pfizer submitted a marketing application to the US FDA in August 2014 and obtained priority review qualifications for estrogen receptor positive (ER+) and human epidermal growth factor receptor 2 negative ( First-line treatment of HER2-) advanced breast cancer. The drug's successful research will provide another important option for patients with metastatic breast cancer. Because the medicine does not yet have a standard Chinese translation, the applica...

Claims

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