亲脂性
生物利用度
铜
催化作用
膜透性
组合化学
化学
药物发现
有机化学
膜
药理学
生物化学
医学
作者
Christian Matheis,Victoria Wagner,Lukas J. Gooßen
标识
DOI:10.1002/chem.201504553
摘要
The late-stage introduction of trifluoromethylthio and trifluoromethylseleno groups is of high interest for drug discovery, because these moieties sharply increase the lipophilicity and membrane permeability of bioactive compounds, thus increasing their bioavailability. Straightforward methods to introduce these important moieties, starting from easily available precursors, are disclosed. The key advantages of the Sandmeyer process are its mild reaction conditions, the use of an inexpensive copper catalyst, and the exceptional functional group tolerance. More information can be found in the Communication by L. J. Gooßen et al. on page 79 ff. The late-stage introduction of trifluoromethylthio and trifluoromethylseleno groups is of high interest for drug discovery, because these moieties sharply increase the lipophilicity and membrane permeability of bioactive compounds, thus increasing their bioavailability. Straightforward methods to introduce these important moieties, starting from easily available precursors, are disclosed. The key advantages of the Sandmeyer process are its mild reaction conditions, the use of an inexpensive copper catalyst, and the exceptional functional group tolerance. More information can be found in the Communication by L. J. Gooßen et al. on page 79 ff.
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