A preparation method of fumagillin amino alcohol

The invention discloses a preparation method of fumagillin amino alcohol shown as a formula I in the specification. The method comprises the following steps: (1) reducing amino acid shown in a formulaII to obtain a compound shown in a formula III; and (2) under the heating condition of a methanol so...

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Hauptverfasser: TANG XIAOYAN, WANG MIN, CHANG BAIYANG, WANG TONGTONG, YANG MENGRUI, ZHOU JIAN
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention discloses a preparation method of fumagillin amino alcohol shown as a formula I in the specification. The method comprises the following steps: (1) reducing amino acid shown in a formulaII to obtain a compound shown in a formula III; and (2) under the heating condition of a methanol solution, carrying out an ammonium salt synthesis reaction on fumagillin and the compound shown in the formula III to obtain fumagillin amino alcohol. The preparation method is short in reaction route and high in synthesis efficiency, the separation and purification steps are reduced, and mass production can be achieved. Meanwhile, the synthesized fumagillin amino alcohol is low in toxicity, can be dissolved and degraded in nature and is good in water solubility. 本发明公开了一种式I所示烟曲霉素胺基醇的制备方法。该方法包括下述步骤:(1)将式II所示的氨基酸进行还原,得到式III所示化合物;(2)在甲醇溶液加热条件下,使烟曲霉素与式III所示化合物经铵盐合成反应,即得。本发明制备方法的反应路线短,合成效率高,减少了分离纯化的步骤,可大量生产。同时合成烟曲霉素氨基醇的毒性低,在自然界溶解降解且水溶性好。