- Preparation method for rifamycin S derivative
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The invention relates to a preparation method for a rifamycin S derivative. According to the preparation method, 3-amino-4-imine rifamycin S as shown in a formula II which is described in the specification and a 4-piperidone derivative as shown in a formula III which is described in the specification are added according to a certain feeding mode and subjected to a condensation reaction in the presence of an organic solvent, ammonium acetate and zinc dust so as to produce the rifamycin S derivative as shown in a formula I which is described in the specification. The feeding mode is that the 3-amino-4-imine rifamycin S is added into a reaction system in a final step, so 3-amino-4-imine rifamycin S is prevented from reduction and hydrolysis. The preparation method increases the utilization rate of materials and is shortened in reaction time, so high-efficiency high-yield preparation of the rifamycin S derivative is realized, and the yield and content of the rifamycin S derivative reach 80% or above and 95% or above, respectively; and the preparation method overcomes the problems of long reaction time, low yield, many impurities and high cost, and is simple to operate, highly efficient, environment friendly and beneficial for large-scale production.
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Paragraph 0035
(2017/08/25)
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- NITROHETEROARYL-CONTAINING RIFAMYCIN DERIVATIVES
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Substituted rifamycin derivatives in which a nitroimidazole, nitrothiazole or nitrofuran pharmacophore is covalently bonded to a rifamycin, methods of using the rifamycin derivatives, and pharmaceutical compositions containing the rifamycin derivatives are disclosed. Methods of synthesizing these substituted rifamycin derivatives are also disclosed. The rifamycin derivatives possess antibacterial activity, and are effective against a number of human and veterinary pathogens in the treatment of bacterial diseases.
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Page/Page column 62
(2010/11/29)
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