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    • 65. 发明授权
    • Electrochemical process for preparing hydroxylaminoeverninomicins
    • 制备羟基氨基炔诺酮的电化学方法
    • US3998708A
    • 1976-12-21
    • US650082
    • 1976-01-19
    • Peter KabasakalianSami Y. KallineyAshit K. GangulyAnita Westcott
    • Peter KabasakalianSami Y. KallineyAshit K. GangulyAnita Westcott
    • C07H19/01C25B3/04C07D325/00C07H15/00
    • C07H19/01C25B3/04
    • Hydroxylaminoeverninomicins having antibacterial activity are prepared by electrochemically reducing the corresponding everninomicin having a nitro function or the corresponding nitrosoeverninomicin in an aqueous miscible organic solvent under an inert atmosphere or in an anhydrous aprotic solvent in the presence of carbon dioxide. Additionally, nitrosoeverninomicins, upon electrochemical reduction in an aprotic solvent under an inert atmosphere, are converted to the corresponding hydroxylaminoeverninomicins. Preferred starting compounds are everninomicins B, C and D whereby are obtained hydroxylaminoeverninomicins B, C and D, respectively. Particularly useful is the electrochemical reduction of everninomicin D in anhydrous dimethylformamide in the presence of carbon dioxide to obtain hydroxylaminoeverninomicin D of excellent purity in high yields.
    • 具有抗菌活性的羟基氨基炔诺酮通过在二氧化碳存在下,在惰性气氛或无水质子惰性溶剂中,在含水混溶性有机溶剂中,电化学还原具有硝基官能团的相应的伊维菌素或相应的亚硝吗啉。 另外,在非质子溶剂中在惰性气氛下电化学还原时,亚硝基毒素被转化为相应的羟基氨基炔诺酮。 优选的起始化合物是乙酰丙酮蛋白B,C和D,分别得到羟基氨基炔诺酮B,C和D。 特别有用的是在二氧化碳存在下在无水二甲基甲酰胺中电解还原everninomicin D,以高产率获得优异的纯度的羟基氨基炔诺酮D。