Compound treating diabetes and relevant complicating diseases and preparation method and application thereof
The technology of a compound and a composition is applied in the field of compounds for the treatment of diabetes and its complications, which can solve the problems of aggravating pancreatic β-cell failure, deterioration of blood quality, diabetes complications, metabolic defects, etc., so as to prevent diabetes and its complications. , The effect of regulating glucose metabolism and lipid metabolism, and repairing diseased blood vessels
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[0061] The present invention further provides the preparation method of above-mentioned compound, and process route and preparation steps are as follows:
[0062] The process route for preparing compound 1 is as follows:
[0063] Preparation of compounds 3 and 4 and 5:
[0064] The furanone acetate can be obtained by reacting acetyl chloride with benzylamine furanone, which is called compound 5.
[0065] The preparation process of compound 2:
[0066] Preparation process: 1.2g (0.01mol) of (E)-3-methoxy-2-methylpropenoate was mixed with 1.3g (0.01mol) of reagent b and heated to 90°C for 2 minutes in a microwave generator to obtain colorless Oily liquid 2. The next reaction was carried out directly without separation.
[0067] HNMR: 5,12(d,1H,OCHO,J 2,3Hz); 4,31-4,16(m,3H,OCH 2 , et NCH) 3,86 (dd, 1H, CHCO, J 7,8Hz, J 2,3Hz); 3,78 (s, 3H, OCH 3 ); 3,44(s, 3H, OCH 3 ); 2,89(s, 3H, NCH 3 ); 1,29(t,3H,CH 2 CH 3 , J 7,1Hz).
[0068] 3 preparation techniques of compou...
Embodiment 1
[0099] The components and parts by weight of the composition are as follows:
[0100] Benzylaminofuranone 10;
[0101] 2-Hydroxypropyl-β-cyclodextrin 20;
[0102] Excipients 150.
[0103] Benzylamine furanone is the main ingredient, mannitol and aspirin lysine are excipients (the dosage should be less than their minimum medicinal dosage), or dextran, lactose, hydrolyzed gelatin trehalose, galactose, xylose can be used Other commonly used excipients such as alcohol, preferably a mixture of mannitol and aspirin lysine in any ratio is the excipient. Among β and γ cyclodextrins, 2-hydroxypropyl-β-cyclodextrin is preferred. tert-butanol as solvent. Or water for injection and other non-toxic solvents, preferably tert-butanol, are used as solvents.
[0104] Preparation Process:
[0105] (1) Dissolve benzylaminofuranone, mannitol, aspirin lysine salt, and 2-β-cyclodextrin in tert-butanol in sequence.
[0106] (2) Use 10%-20% aqueous solution of lactic acid / sodium lactate or cit...
Embodiment 2
[0127] The components and parts by weight of the composition are as follows:
[0128] Benzylaminofuranone 50;
[0129] Excipient 300;
[0130] 2-Hydroxy-β-cyclodextrin 100.
[0131] Benzylamine furanone is the main ingredient, mannitol and aspirin lysine are excipients (the dosage should be less than their minimum medicinal dosage), or dextran, lactose, hydrolyzed gelatin trehalose, galactose, xylose can be used Other commonly used excipients such as alcohol, preferably a mixture of mannitol and aspirin lysine in any ratio is the excipient. Among β and γ cyclodextrins, 2-hydroxypropyl-β-cyclodextrin is preferred. tert-butanol as solvent. Or water for injection and other non-toxic solvents, preferably tert-butanol, are used as solvents.
[0132] Preparation Process:
[0133] (1) Dissolve benzylaminofuranone, mannitol, aspirin lysine salt, and 2-β-cyclodextrin in tert-butanol in sequence.
[0134] (2) Use 10%-20% aqueous solution of lactic acid / sodium lactate or citric ac...
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