Zatosetron maleate is a potent, selective 5-hydroxytryptamine receptor antagonist. In anticipation of commercialization, a manufacturing synthesis of zatosetron from tropinone and 5-chlorosalicylic acid was developed. Development efforts focused on addressing several key issues including the supply and quality of the critical raw material tropinone, improvements in the stereoselective formation of 3-endo-tropanamine, and the compatibility with existing manufacturing capabilities of process requirements for the Claisen rearrangement used to produce a crucial benzofuran intermediate. The results of these studies and an improved route to zatosetron maleate are described.

中文翻译：

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马来酸Zatosetron制造工艺的开发

马来酸Zatosetron是一种有效的选择性5-羟色胺受体拮抗剂。为了期待商品化，开发了由肌钙蛋白和5-氯水杨酸的合成制备泽托司琼的方法。开发工作的重点是解决几个关键问题，包括关键原料肌钙蛋白的供应和质量，3-内-三聚泛胺的立体选择性形成的改进以及与用于生产苯丙胺的克莱森重排的工艺要求与现有制造能力的兼容性。至关重要的苯并呋喃中间体。描述了这些研究的结果和改进的马来酸佐斯托琼的途径。