发明名称 METHOD FOR PREPARING 3-AZIDO-DERIVATIVES OF RIFAMYCIN S
摘要 FIELD: organic chemistry, chemical technology, antibiotics. ^ SUBSTANCE: invention relates to methods for preparing derivatives of 3-aazidorifamycin S eliciting antibiotic properties. Method for preparing 3-azido-derivatives of rifamycin S involves interaction rifamycin S derivative with hydrazoic acid salt in solvent medium by stirring reagents at temperature from 0oC to 100oC for 0.5-2 h followed by extraction of the end product. 3-Halogen-derivative of rifamycin S is used as rifamycin S derivative. Simple aliphatic alcohols with carbon atom number from 1 to 5 or acetonitrile, or mixture of water and organic solvent not mixing with water taken among the series: ethyl acetate, methyl acetate, benzene or its mono- or dimethyl analogues, chlorinated hydrocarbons with carbon atom number from 1 to 3 is used as a solvent. Sodium azide or potassium azide is used as hydrazoilc acid salt. Extraction of the end product is carried out by extraction with solvent not mixing with water or by dilution of reaction mixture with water followed by filtration. The claimed method provides enhancing the yield of the end product by 63-71% and to simplify the process of it isolating. Invention provides the enhancement of effectiveness of method for preparing 3-azido-derivatives of rifamycin S due to elevating yield of the end product and simplifying the process of its isolating. ^ EFFECT: improved preparing method. ^ 1 tbl, 13 ex
申请公布号 RU2245337(C2) 申请公布日期 2005.01.27
申请号 RU20020126552 申请日期 2002.09.27
申请人 发明人 OVCHINNIKOV D.V.;POLUKEEV V.A.
分类号 C07D498/08 主分类号 C07D498/08
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