产量(工程)
腈
水解
酰胺
比例(比率)
组合化学
敌手
立体化学
化学
材料科学
有机化学
受体
物理
冶金
生物化学
量子力学
作者
Raffael Davenport,Florence Masse,Alice Prud’homme,Cédric Bürki,Patric Doerrwaechter,Marco Künzli,Fabio D’Aiuto,Martin H. Bolli,Gabriel Schäfer
标识
DOI:10.1021/acs.oprd.3c00423
摘要
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.
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