Diosmin Synthesis Using Amide Solvents
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Solution Overview
Problem
Current methods for preparing Diosmin involve the use of toxic and difficult-to-remove solvents like pyridine, leading to high solvent residues and environmental and health hazards, while also resulting in low purity and high production costs due to the low content of Diosmin in natural plants.
Innovation Solution
A method using an amide solvent, such as dimethylformamide, in combination with hesperidin and iodine, under controlled pH and temperature conditions, to achieve a high-purity Diosmin synthesis with reduced solvent residue and improved environmental safety.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If pyridine or morpholine is used as reaction solvent, then the Diosmin synthesis reaction can proceed, but the solvent residue in the product is high and the toxicity increases
Solution Approach 1:
The patent changes the solvent parameter from traditional pyridine/morpholine to amide solvents (DMF, DMAc, NMP), which have different chemical properties including lower toxicity and better removability, while maintaining reaction effectiveness
Solution Approach 2:
The patent employs solvents that are easier to remove completely from the product, treating the solvent as a temporary medium that should be fully eliminated rather than remaining in the final product, thereby reducing residue and toxicity
2Reliability
If direct extraction from natural plants is used, then Diosmin can be obtained, but the cost is extremely high due to low content
Solution Approach 1:
The patent changes the production approach from direct natural extraction to chemical synthesis via hesperidin oxidation, fundamentally altering the manufacturing parameter to achieve cost reduction while maintaining product obtainability
3Productivity
If pyridine is used as main solvent, then the reaction can be performed, but the harm to environment and personnel is obvious due to irritant odor and toxic effect
Solution Approach 1:
The patent changes the solvent chemical composition parameter to amide-based solvents that possess lower volatility and reduced toxicity, thereby maintaining reaction productivity while eliminating harmful odors and health risks associated with pyridine
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The method achieves a high yield of up to 85% Diosmin with HPLC purity exceeding 92.5%, minimizing solvent residue and toxicity, and is environmentally friendly, reducing production costs and health risks.
Implementation Method 1
mixing an amide solvent, hesperidin, an alkaline reagent and iodine, and performing a heating reaction to obtain Diosmin
Implementation Method 2
mixing an amide solvent, hesperidin and an alkaline reagent to obtain a raw material solution
Implementation Method 3
performing a heating reaction to obtain Diosmin
Implementation Method 4
recovering solvent under reduced pressure after heating reaction
Data Source
AI summary
A method for preparing Diosmin is provided in the present invention, comprising: A) mixing amide solvents, hesperidin, alkaline reagents and iodine, and performing heating reaction to obtain Diosmin. Compared with the prior art, amide solvents are used as reaction solvents in the present invention, which are less toxic and soluble in water, and easy to be processed, so that the residual amount of solvents in the obtained product is reduced.