Optimization of a Kilogram-Scale Synthesis of a Potent Cycloartenol Triterpenoid-Derived 纬-Secretase Modulator

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• 作者：Nathan O. Fuller ; Jed L. Hubbs ; Wesley F. Austin ; Ruichao Shen ; Jeffrey Ives ; Gerd Osswald ; Brian S. Bronk
• 刊名：Organic Process Research & Development
• 出版年：2014
• 出版时间：June 20, 2014
• 年：2014
• 卷：18
• 期：6
• 页码：683-692
• 全文大小：441K
• 年卷期：v.18,no.6(June 20, 2014)
• ISSN：1520-586X

文摘

This work describes the demonstration of a kilogram-scale synthesis of a 纬-secretase modulator from a plant-sterol-derived starting material. Key to developing a synthetic route capable of delivering a kilogram of the target compound was the development of a four-reaction telescope process and a selective O-alkylation of a triol intermediate. These improvements enabled the successful delivery of kilogram-scale batches of API for preclinical development studies.