Arbekacin synthesis method
A technology of arbekacin and synthetic method, which is applied in the field of synthesis of aminoglycoside antibiotics, can solve the problems of product stability impact, product stability impact, poor selectivity, etc., and achieve easy industrial production, reduce production cost, and yield Improved effect
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Embodiment 1)
[0021] (a) Synthesis of 3,2',6'-tri-N-tert-butoxycarbonyl-3',4'-dideoxykanamycin B:
[0022] Dissolve 1 g of 3',4'-dideoxy-3',4' didehydro-kanamycin B (dibekacin) and 30 g of dimethylformamide (DMF), add zinc acetate, fully Stir to complete the complexation; put in 1.2 grams of di-tert-butyl dicarbonate, react for 1 hour, and determine the end point by TLC;
[0023] Then the reaction solution was diluted with water, and the filtrate was adsorbed on the cation exchange [NH 4 + ]-type resin column, after washing with a large amount of water, elute with ammonia water, collect the components with three protected compounds, and concentrate to dryness under reduced pressure to obtain a yellow solid 3,2',6'-tri-N-tert-butoxycarbonyl -3'.4'-Dideoxy-3',4'Didehydro-Kanamycin B;
[0024] (b) Synthesis of 1-tert-butoxyamido-3-hydroxybutyric acid
[0025] In an aqueous solution of 1.74 grams of sodium bicarbonate and 56 grams of 1,4-dioxane, add 2.25 grams of 2-hydroxy-4-aminobutyric a...
Embodiment 2)
[0033] (a) Synthesis of 3,2',6'-tri-N-tert-butoxycarbonyl-3',4'-dideoxykanamycin B:
[0034] Dissolve 1 g of 3',4'-dideoxy-3',4' didehydro-kanamycin B (dibekacin) and 30 g of dimethylformamide (DMF), add C1-5 carboxyl The divalent transition metal zinc acetate of the acid is fully stirred to make it complexed completely; drop into 1.2 grams of di-tert-butyl dicarbonate, react for 1 hour, and determine the end point by TLC;
[0035] Then the reaction solution was diluted with water, and the filtrate was adsorbed on the cation exchange [NH 4 + ]-type resin column, after washing with a large amount of water, elute with ammonia water, collect the components with three protected compounds, and concentrate to dryness under reduced pressure to obtain a yellow solid 3,2',6'-tri-N-tert-butoxycarbonyl -3'.4'-Dideoxy-3',4'Didehydro-Kanamycin B;
[0036] (b) Synthesis of 1-tert-butoxyamido-3-hydroxybutyric acid
[0037] In an aqueous solution of 1.74 grams of sodium bicarbonate and 56...
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