Composite catalyst and its use in the synthesis of substituted benzimidazole derivatives

By using a melt synthesis method involving the reaction of a composite catalyst with o-phenylenediamine and haloaromatic acids at high temperature, substituted benzimidazole derivatives have been synthesized, solving the problems of low purity and yield in existing technologies and achieving efficient and environmentally friendly industrial production.

CN117816164BActive Publication Date: 2026-06-09INST OF CHEM ENG GUANGDONG ACAD OF SCI
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
INST OF CHEM ENG GUANGDONG ACAD OF SCI
Filing Date
2022-09-29
Publication Date
2026-06-09

AI Technical Summary

Technical Problem

Existing methods for synthesizing substituted benzimidazole derivatives have low product purity and yield, making industrial-scale production difficult.

Method used

Using composite catalysts Fe/Na2B4O7, Fe/B2O3, Na2SO3/Na2B4O7, Na2SO3/B2O3, SnCl2/Na2B4O7, or SnCl2/B2O3, substituted benzimidazole derivatives are synthesized via a melt method by reacting with o-phenylenediamine and haloaromatic acids at high temperature under inert gas protection. This avoids the oxidation of o-phenylenediamine and promotes the closure of the imidazole ring.

Benefits of technology

It significantly improves the yield of substituted benzimidazole derivatives to over 95% and the purity to over 99%, simplifies the process, is environmentally friendly, and is suitable for industrial production.

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Abstract

The application discloses a composite catalyst and application thereof in synthesis of substituted benzimidazole derivatives, and belongs to the technical field of organic synthesis. The composite catalyst is one or several of Fe / Na2B4O7, Fe / B2O3, Na2SO3 / Na2B4O7, Na2SO3 / B2O3, SnCl2 / Na2B4O7 or SnCl2 / B2O3. The composite catalyst is applied to the synthesis of substituted benzimidazole derivatives by a melting method, so that the yield of a crude product can be obviously improved to more than 95 %, and the purity of the purified substituted benzimidazole derivatives can reach more than 99 %, so that the substituted benzimidazole derivatives can be prepared at a high yield and high purity.
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