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发明授权
CN101235081B 缩宫素的制备方法 有权 质押 转让

缩宫素的制备方法
摘要：
本发明公开了一种缩宫素的制备方法。该方法先分别合成中间体a和中间体b，然后以叠氮基磷酸二苯酯为缩合剂，在DMF、DPPA、二氧六环、哌啶、TFA及DCM存在的条件下，以中间体a和中间体b进行反应，控制反应温度-20～40℃，反应10～40小时，在通入空气氧化反应完成后，经真空干燥除去反应体系中的溶剂，得到缩宫素。本发明具有肽链接完全、纯化简单易行、收率高、目标产物缩宫素的光学活性及化学纯度高的优点。
摘要（英）：

The invention discloses an oxytocin preparation method, comprising respectively synthesizing an intermediate a and an intermediate b, using diphenyl azidophopshate as condensing agent, in the presence of DMF, DPPA, dioxane, piperidine, TFA and DCM, reacting intermediate a with intermediate b, controlling the reaction temperature at -20 to 40 DEG C and reaction time of 10-40h, feeding air, after the oxidization, drying in vacuum to remove the solvent in the reaction system to obtain oxytocin. The invention has complete connected peptide chain, simple purification, simple process, high yield, optical activity and chemical purity of target product oxytocin.

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