A continuous flow method for the synthesis of a boscalid derivative

By employing a continuous flow synthesis method using a microchannel reactor, the problems of explosion risk and low yield in the synthesis of Bosein derivatives have been solved, achieving safe and efficient preparation of Bosein derivatives with improved yield and better environmental friendliness.

CN120717986BActive Publication Date: 2026-04-28KUNMING UNIV OF SCI & TECH
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Patent Information

Application Number
CN202510742107.1
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2025-06-05
Publication Date
2026-04-28
Estimated Expiration
2045-06-05

AI Technical Summary

Technical Problem

Existing synthesis processes for Bosein derivatives pose an explosion risk and have low yields, making it difficult to meet safety and environmental protection requirements.

Method used

A continuous flow synthesis method using a microchannel reactor was employed to synthesize 2,4(1H,3H)-pyrimidinidone-5-D-glucopyranosyl-6-hydroxy-1,3-dimethyl sodium salt under alkaline conditions via a two-step reaction. This salt was then reacted with an oxidant in another microchannel reactor to yield (2ξ,3ξ)-3,7-dehydro-N-methyl-D-glucosinolate. Subsequent alkalization, esterification protection, and lactone formation steps yielded a series of Bosein derivatives.

Benefits of technology

A safe and efficient synthesis of Bosein derivatives was achieved, increasing the yield from 61.7% to 78%, simplifying the operation process, reducing environmental pollution, and improving product purity and yield.

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Abstract

The application provides a continuous flow synthesis method of a Bose factor derivative, which comprises flowing reaction of D-glucose and dimethyl barbituric acid under alkaline conditions in a micro-channel reactor to synthesize 2,4(1H,3H)-pyrimidine dione-5-D-glucopyranosyl-6-hydroxy-1,3-dimethyl sodium salt, and flowing reaction of the reaction product with an oxidizing agent in another micro-channel reactor to obtain the Bose factor derivative (2ξ,3ξ)-3,7-dehydrated-N-methyl-D-glucosinamide. The continuous synthesis method of the Bose factor derivative has the advantages of short reaction time, simple operation, high automation degree, cheap and easily obtained reagent, high purity of the obtained product, and few impurities. Meanwhile, the preparation method has the advantages of high safety, large production capacity, high yield, reduced environmental pollution, and good application prospect.
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