Synthesis method of abesilib intermediate
By using an oxidant and hydrochloric acid treatment in a specific solvent, combined with the reaction of acyl chloride reagents and base, a high-yield, high-purity abemaciclib intermediate was successfully prepared, solving the problems of low yield and low purity in the existing technology and realizing green and environmentally friendly industrial production.
CN120682157APending Publication Date: 2025-09-23SUNSHINE LAKE PHARMA CO LTD
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Patent Information
- Application Number
- CN202510706287.8
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2025-05-29
- Publication Date
- 2025-09-23
AI Technical Summary
Technical Problem
The existing synthesis methods of abemaciclib intermediates have the problems of low yield, low purity, harsh reaction conditions and unsuitability for industrial production.
Method used
An oxidative ring-closure reaction is carried out using an oxidant in a specific solvent, followed by treatment with hydrochloric acid and a reaction of an acyl chloride reagent with a base to prepare compounds R0-02 and R0-03, which are finally mixed with an alkaline reagent aqueous solution to precipitate compound R0-04.
Benefits of technology
The yield and purity of the abemaciclib intermediate are improved, the use of strong base and high temperature is avoided, the operation process is simplified, and the cost is reduced.
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Abstract
The invention relates to a synthesis method of an abelsilil intermediate, and belongs to the field of chemistry. The method comprises at least one of synthesis of N-(4-bromine-2-fluorophenyl)-N '-(1-methyl ethyl) acetamidine, synthesis of 6-bromine-4-fluoro-1-isopropyl-2-methyl-1H-benzo [d] imidazole hydrochloride, and preparation of 6-bromine-4-fluoro-1-isopropyl-2-methyl-1H-benzo [d] imidazole. The preparation method comprises the following steps: synthesizing N-(4-bromine-2-fluorophenyl)-N'-(1-methyl ethyl) acetamidine, synthesizing 6-bromine-4-fluoro-1-isopropyl-2-methyl-1H-benzo [d] imidazole hydrochloride, and preparing 6-bromine-4-fluoro-1-isopropyl-2-methyl-1H-benzo [d] imidazole. According to the method provided by the invention, potassium tert-butoxide is not adopted as alkali, impurities with tert-butanol are not introduced, strong alkali is not used, ring closing is carried out at high temperature, the method is green and environment-friendly, the method provided by the invention is simple in post-treatment and high in yield, the obtained product is high in purity, and cost reduction is facilitated. The product prepared by the method provided by the invention has the advantages of high yield, high purity, mild reaction and simple operation. The adopted materials are cheap, easy to obtain and low in cost.
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