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PROCESS FOR PRODUCING O-ALKYLATED RAPAMYCIN DERIVATIVE, AND O-ALKYLATED RAPAMYCIN DERIVATIVE
PROCESS FOR PRODUCING O-ALKYLATED RAPAMYCIN DERIVATIVE, AND O-ALKYLATED RAPAMYCIN DERIVATIVE
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机译:O-烷基化雷帕霉素衍生物和O-烷基化雷帕霉素衍生物的生产方法
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摘要
A process for producing an O-alkylated rapamycin derivative of high purity, i.e. a purity is not lower than 99%, is porivided.;A process for producing an o-alkylated rapamycin derivative represented by the following general formula (1) is provided. The process includes the steps of reacting rapamycin with an alkyl triflate, purifying a reaction product, which has been obtained by the above reaction, with a normal phase chromatograph and further purifying a purified product, which has been purified with the normal phase chromatograph, with a reverse phase chromatographwherein R represents alkyl, arylalkyl, hydroxyalkyl, alkoxyalkyl, acyloxyalkyl, aminoalkyl, alkylaminoalkyl, alkoxycarbonylaminoalkyl, acylaminoalkyl, or aryl.
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机译:制备高纯度即纯度不低于99%的O-烷基化雷帕霉素衍生物的方法。提供了一种由以下通式(1)表示的O-烷基化雷帕霉素衍生物的制备方法。该方法包括以下步骤:使雷帕霉素与三氟甲磺酸烷基酯反应,用正相色谱仪纯化通过上述反应获得的反应产物,并进一步纯化用正相色谱仪纯化的纯化产物。反相色谱仪 <图像文件=“ IMGA0001.GIF” he =“ 68” imgContent =“ chem” imgFormat =“ GIF” wi =“ 92” /> Chemistry>其中R代表烷基,芳基烷基,羟烷基,烷氧基烷基,酰氧基烷基,氨基烷基,烷基氨基烷基,烷氧基羰基氨基烷基,酰基氨基烷基或芳基。
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