Tulathromycin intermediate, preparation method of tulathromycin intermediate and preparation method of tulathromycin
A telamycin and intermediate technology, applied in the field of veterinary antibiotics, can solve the problems of expensive raw materials and harsh reaction conditions, and achieve the effects of reducing production costs, easy separation, and cost reduction
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[0038] The synthetic method steps of telamycin intermediate and telamycin among the present invention are as follows:
[0039] 1. Synthesize key intermediates through protection, oxidation, epoxidation, deprotection, Beckmann rearrangement and reduction hydrolysis of erythromycin A(E) oxime;
[0040] 2. Put the telamycin intermediate and n-propylamine in isopropanol and use magnesium bromide as a catalyst to obtain telamycin that meets the quality standards. Its specific reaction route figure 1 shown.
Embodiment
[0042] Add erythromycin A(E) oxime (50 g, 0.067 mol), pyridine (5 g, ), dichloromethane (500 mL) into a 1L round-bottomed flask, stir vigorously in an ice-water bath, and slowly add acetic anhydride (16 mL , 0.17 mol) for about 45 min, TLC detection and reaction for 6 h, suction filtration, and drying to obtain a white solid, namely intermediate 1, with a yield of 100%.
[0043] Add intermediate 1 (50 g, 0.06 mol) into a 2L three-neck flask, protect it under nitrogen, inject DMSO (170 mL), heat to 60°C, slowly add acetic anhydride (110 mL, 1.2 mol) dropwise for about 1 hour, and maintain 60°C After reacting for 2 hours, after cooling, 100 mL of methanol was added to quench the reaction, concentrated under reduced pressure, a solid precipitated out, and dried to obtain a white solid, namely intermediate 2, with a yield of 90%.
[0044] Add trimethylsulfonium bromide (16.5 g, 0.11 mol) and anhydrous tetrahydrofuran (200 mL) into a 1L three-necked flask, cool to -20°C, add sodium h...
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