A preparation method of abemaciclib

By improving the preparation method of abecili, 6-bromo-4-fluoro-1-isopropyl-2-methyl-1H-benzimidazole is used as the starting material, and abecili is generated through a series of specific chemical reactions, which solves the problems of difficulty in recycling, high cost and high environmental protection treatment pressure in the prior art, and achieves a safe and green preparation process and high purity products.

CN119751416APending Publication Date: 2025-04-04CHONGQING SHENGHUAXI PHARMA CO LTD +1
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Patent Information

Application Number
CN202411968679.3
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2024-12-30
Publication Date
2025-04-04

AI Technical Summary

Technical Problem

There are problems such as difficulty in recycling, high cost, high environmental protection treatment pressure and difficult impurity control in the existing Abecili preparation method.

Method used

6-bromo-4-fluoro-1-isopropyl-2-methyl-1H-benzimidazole was used as the starting material, and the intermediate was reacted with Weber amide after activation of isopropyl magnesium bromide, followed by reaction with N,N-dimethylformamide dimethylacetal and guanidine hydrochloride, and finally reacted with intermediate-b under the action of palladium catalyst and phosphorus-containing ligand to form abecili.

Benefits of technology

Abelcili has been achieved safe and green preparation, reducing costs, simplifying the recycling process, reducing environmentally friendly processing pressure, effectively controlling impurities, and improving the purity of the product.

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Abstract

The invention discloses a preparation method of abemaciclib. The abemaciclib involved in the invention uses 6-bromo-4-fluoro-1-isopropyl-2-methyl-1H-benzimidazole as a starting material, is first activated with isopropylmagnesium bromide, reacts with 2-fluoro-N-methoxy-N-methylacetamide, then reacts with DMFDMA, and cyclizes with guanidine hydrochloride, and finally catalytically couples with an intermediate b to obtain abemaciclib. The preparation method has easy-to-obtain raw materials, low cost, few side reactions, and is safe and environmentally friendly.
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