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Liquid Assisted Grinding for the N-Demethylation of Alkaloids
ACS Sustainable Chemistry & Engineering ( IF 7.1 ) Pub Date : 2018-06-21 00:00:00 , DOI: 10.1021/acssuschemeng.8b01393
Jon Kyle Awalt 1 , Peter J. Scammells 2 , Robert D. Singer 1
Affiliation  

A mechanochemical approach has been demonstrated for the selective cleavage of nitrogen–carbon bonds in the N-demethylation of various alkaloids relevant in the pharmaceutical industry. This methodology employs a range of so-called “liquid additives” used in microliter quantities in liquid assisted grinding rather than “solvents” used in solution phase reactions. Green liquid additives such as alcohols, water, PEG and ionic liquids as well as a nonchemical, mechanical approach for the generation of nanoscale Fe0 dust significantly improve the green attributes of the N-demethylation process.

中文翻译:

液体辅助研磨生物碱的N-去甲基化

已经证明了一种机械化学方法可以选择性地裂解与制药工业相关的各种生物碱的N-脱甲基化过程中的氮碳键。该方法采用了一系列在液体辅助研磨中以微升使用的所谓“液体添加剂”,而不是在溶液相反应中使用的“溶剂”。绿色液体添加剂(例如醇,水,PEG和离子液体)以及用于生成纳米级Fe 0粉尘的非化学机械方法显着改善了N-去甲基化过程的绿色特性。
更新日期:2018-06-21
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