Development of a Practical Process for the Opening of Macrocyclic Cyclosporin A and Amino Acid Deletion

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• 作者：Bernard Riss ; Arnaud Grandeury ; Thorsten Gut ; Manuela Seeger-Weibel ; Christian Zuercher ; Jinjing Li ; Fabrice Gallou
• 刊名：Organic Process Research & Development
• 出版年：2014
• 出版时间：December 19, 2014
• 年：2014
• 卷：18
• 期：12
• 页码：1763-1770
• 全文大小：443K
• ISSN：1520-586X

文摘

A practical and robust process for the derivatization of Cyclosporin A was demonstrated. The processes rely on the opening of Cyclosporin A and removal of amino acid fragments via Edman degradation, with the isolation of crystalline tetrafluoroboric salts of the corresponding acyclic polypeptides.