首页> 外国专利> Isolation of ergol-type peptide alkaloid(s) - from rye ergot drugs and Claviceps purpurea cultures, by dissolution in a protic solvent, separation of precipitated epimers and defatting

Isolation of ergol-type peptide alkaloid(s) - from rye ergot drugs and Claviceps purpurea cultures, by dissolution in a protic solvent, separation of precipitated epimers and defatting

机译:通过溶解在质子溶剂中,分离沉淀的差向异构体和脱脂,从黑麦麦角药和紫薇培养物中分离出麦角酚型肽生物碱

摘要

Process for isolating peptidic alkaloids of the ergol type, from rye ergot drugs or from submerged cultures of Claviceps purpurea, by extraction and purification of the extract by changing the phase comprises (a) dissolving the crude mixt. of ergot-type peptidic alkaloids in a protic solvent, partic. 1-6C alkanols; (b) sepn. of the precipitated epimers; (c) defatting with a fat solvent, partic. MIBK or butyl acetate and (d) preparing the obtd. prod. Used for isolation of therapeutically-active peptidic alkalids having ergot structure e.g. ergotamine, the three ergotoxine alkaloids, ergocristine, ergocornine and ergocryptine and intermediates for rye ergot dihydroalkaloids. Simple process is suitable for industrial scale production and reduces the number of phase changes in known processes and yields a crystalline (not amorphous) product. The extraction stage with the protic solvent gives an almost quantitative recovery of the dextro-rotatory form. The defatting stage gives a high purity product which can be used in medicament formulations without further purification.
机译:通过提取和通过改变相来纯化提取物,从黑麦角麦角蛋白或紫红色的克拉维氏菌的深层培养物中分离出麦角型肽生物碱的方法,该方法包括(a)溶解粗混合物。质子溶剂,特别是麦角型肽生物碱的合成1-6C链烷醇; (b)9月。沉淀的差向异构体; (c)用脂肪溶剂脱脂,特别是。 MIBK或乙酸丁酯和(d)制备obtd。产品用于分离具有麦角结构的治疗活性肽碱,例如麦角胺,三种麦角碱生物碱,麦角新碱,麦角碱和麦角隐碱以及黑麦麦角二氢生物碱的中间体。简单的工艺适合于工业规模生产,并减少了已知工艺中的相变次数,并产生了结晶(非非晶)产物。用质子溶剂萃取的步骤几乎可以定量回收右旋旋转形式。脱脂阶段得到高纯度的产物,其无需进一步纯化即可用于药物制剂。

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