Process Development of the Synthesis and Purification of a Reactive Immuno-PET Conjugate Intermediate

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• 作者：Diane E. Carrera ; Tina Nguyen ; Colin Medley ; Yi Li ; Remy Angelaud ; Francis Gosselin
• 刊名：Organic Process Research & Development
• 出版年：2016
• 出版时间：February 19, 2016
• 年：2016
• 卷：20
• 期：2
• 页码：312-318
• 全文大小：356K
• ISSN：1520-586X

文摘

We describe a practical multigram scale synthesis of the reactive immuno-PET linker-chelator GNE-605 from the commercially available starting material desferrioxamine B mesylate. A modified three-step synthetic procedure was developed that significantly reduces the amount of solvents and reagents required as compared to previous literature. Additionally, due to the unique handling challenges posed by this reactive intermediate, a liquid chromatography purification and lyophilization procedure was developed to allow for the first isolation of GNE-605 as a solid material.