91177-27-4Relevant academic research and scientific papers
Preparation method of oxacephem mother nucleus
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Paragraph 0032-0041, (2019/08/17)
The invention discloses a preparation method of oxacephem mother nucleus. the method comprises the following steps: using a compound (I) as a raw material, firstly carrying out an oxidization reactionbetween the compound (I) and peroxide in an organic solvent, then letting the reaction product react with sodium thiosulfate, extracting a dichloromethane phase after the reaction, carrying out negative pressure distillation, and adding a crystallization solvent to obtain the final product oxacephem mother nucleus. The preparation method of the oxacephem mother nucleus has the following advantages: the preparation operation is simple; the raw materials for the preparation are cheap and easily available; the preparation cost is low; the reaction route is short; molar yield is high; the preparation method is easy for industrialization; and the purity of the prepared finished product (HPLC) can reach 99%.
Synthesis method of oxacephem nucleus
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Paragraph 0035; 0039; 0043; 0047; 0048-0049; 0054-0057, (2019/04/06)
The invention discloses a synthesis method of oxacephem nucleus. The method comprises the steps: dissolving 1-oxycephalosporin-3-methylene (001) as a raw material by taking dichloromethane as a solvent, then, slowly introducing hydrogen chloride and oxygen after the raw material is dissolved, ending a reaction, regulating the pH value of a reaction feed liquid to 5.0-7.0 by using a sodium hydrogencarbonate solution with the mass percentage being 5%, carrying out extraction to obtain a dichloromethane phase, carrying out reduced pressure distillation, then, adding a crystal solvent to obtain oxacephem nucleus serving as a final product. The synthesis method disclosed by the invention is short in step, easy to realize, capable of omitting chlorine serving as a hazardous gas, little in environment pollution, high in process safety, high in product mole yield reaching up to 97% and suitable for industrial production.
Design, synthesis and antibacterial activity of novel 1-oxacephem analogs
He, Yi,Wu, Jian Bo,Lei, Fan,Chen, Pei,Hai, Li,Wu, Yong
, p. 407 - 410 (2012/05/20)
A series of 1-oxacephem analogs were synthesized and their antibacterial properties against five strains of Gram-positive and Gram-negative bacteria were evaluated in vitro while ceftazidine was selected as control. Some of the tested compounds, compound 12c in particular, showed more active against three selected strains than the standard.
