Preparation process of dabigatran etexilate intermediate

Through a new preparation process, including carbonyl activation, amide reaction and cyclosynthesis reaction, combined with the reduced pressure distillation and crystallization steps, the DABB-12 seed crystal was induced, which solved the problem of low purity of the dabigatran ester intermediate in the prior art, and achieved the preparation of a high-purity dabigatran ester intermediate, which was suitable for industrial production.

CN119707928APending Publication Date: 2025-03-28ANHUI MENOVO PHARM CO LTD
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Patent Information

Application Number
CN202411927073.5
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2024-12-25
Publication Date
2025-03-28

AI Technical Summary

Technical Problem

The existing preparation process of dabigatran ester intermediates is difficult to ensure the high purity of the product, and the traditional solvent extraction method is easily disturbed by solvent residues and impurities, affecting the quality of the product.

Method used

A new preparation process is adopted, through carbonyl activation, amide reaction and cyclosynthesis, combined with the reduced pressure distillation and crystallization steps, the crystallization process is controlled to improve the purity of the product.

Benefits of technology

The high purity preparation of dabigatran ester intermediate is achieved, with a purity of more than 97%, which is suitable for industrial production, and reduces the waste of raw materials and the presence of impurities and defects.

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Abstract

The invention discloses a preparation process of a dabigatran etexilate intermediate, and belongs to the field of pharmaceutical chemicals, the prepared intermediate is N-[[z-[[[4-(aminoimino methyl) phenyl] amino] methyl]-1-methyl-1H-benzimidazole-5-yl] carbonyl]-N-2-pyridyl-beta-alanine ethyl ester hydrochloride, and the purity is not less than 98.0%. According to the preparation process, dichloromethane is used as a solvent, 3-[(3-amino-4-methylaminobenzoyl) pyridine-2-ylamino] ethyl propionate, N-(4-cyanophenyl) glycine, imidazole hydrochloride and N, N-carbonyldiimidazole are subjected to a reaction to prepare 3-[(3-amino-4-methylaminobenzoyl) pyridine-2-ylamino] ethyl propionate, and the preparation process is mild in condition, convenient and simple to operate, high in yield and suitable for industrial production. The prepared dabigatran etexilate intermediate has high purity and is suitable for industrial production.
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