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Large-Scale Synthesis of LPA1-Receptor Antagonist ACT-1016-0707
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2024-02-05 , DOI: 10.1021/acs.oprd.3c00423 Raffael Davenport 1 , Florence Masse 1 , Alice Prud’homme 1 , Cédric Bürki 1 , Patric Doerrwaechter 1 , Marco Künzli 1 , Fabio D’Aiuto 1 , Martin H. Bolli 1 , Gabriel Schäfer 1
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2024-02-05 , DOI: 10.1021/acs.oprd.3c00423 Raffael Davenport 1 , Florence Masse 1 , Alice Prud’homme 1 , Cédric Bürki 1 , Patric Doerrwaechter 1 , Marco Künzli 1 , Fabio D’Aiuto 1 , Martin H. Bolli 1 , Gabriel Schäfer 1
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The development and execution of the large-scale synthesis of LPA1-antagonist ACT-1016-0707 is described. Key developments were an improved nitrile hydrolysis, a high-yielding, safe, and easy-to-perform amide coupling, and the isolation and purification of several, previously oily intermediates as crystalline solids. The yield of the longest linear synthesis sequence of nine steps was 34% on a 450 g scale with respect to the final product.
中文翻译：
LPA1 受体拮抗剂 ACT-1016-0707 的大规模合成
描述了 LPA1 拮抗剂 ACT-1016-0707 大规模合成的开发和实施。关键的进展是改进的腈水解、高产、安全且易于执行的酰胺偶联，以及将几种以前的油状中间体分离和纯化为结晶固体。九个步骤的最长线性合成序列的产率为 450 g 规模的最终产物的 34%。
更新日期：2024-02-05
中文翻译：
LPA1 受体拮抗剂 ACT-1016-0707 的大规模合成
描述了 LPA1 拮抗剂 ACT-1016-0707 大规模合成的开发和实施。关键的进展是改进的腈水解、高产、安全且易于执行的酰胺偶联，以及将几种以前的油状中间体分离和纯化为结晶固体。九个步骤的最长线性合成序列的产率为 450 g 规模的最终产物的 34%。
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