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Process Development of a Suzuki Reaction Ud in the Manufacture of Lanabecestat 期刊名称： Organic Process Rearch & Development
travian作者： Ashworth, Ian W.,Campbell, Andrew D.,Cherryman, Janette H.,Clark,
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Jemma,Crampton, Alex,Eden-Rump, Edward,Evans, Matthew,Jones, Martinjavdog com
新时代美容美发F.,Abbas, Sahar,Meadows, Rebecca E.,Skilling, Kathryn,Whittaker,
David,Woodward, Robert,Inglesby, Phillip
年份： 2018年
延世母亲节快乐英语关键词： lanabecestat;manufacture;scavenger;kinetics;Suzuki;process
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摘要：We developed a scalable Suzuki processfor the synthesis of lanabecestat(+)-camsylate, an active pharmaceutical ingredient that was recentlyinvestigated in a Pha III clinical program for the tre棉白杨
atment ofearly Alzheimer's dia. The evolution of this process culminatedwith the u of a stable and crystalline diethanolamine boronic esterthat rapidly hydrolys under the reaction conditions. Herein, wereport that the liberated diethanolamine plays
an important role inthe catalytic process, with supporting evidence for an equilibriumbetween an unbound and bound palladium complex. Additionally, thediethanolamine acts as an internal scavenger during the crystallizationof lanabecestat by increasing the solubility of the palladium species,obviating the need for a discrete scavenging step.
指责英文内容由中国教育图书进出口有限公司引进
