کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
17834 | 42699 | 2008 | 6 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Two lipase-catalyzed sequential synthesis of drug derivatives in organic media Two lipase-catalyzed sequential synthesis of drug derivatives in organic media](/preview/png/17834.png)
The study first reported the efficient lipase catalysis of aza-Markovnikov addition of N-heterocycles to vinyl esters in organic media. After screening the enzyme sources and organic solvents, the yield was up to 82.6% and the reaction rate increased more than 600-folds under the catalysis of Amino lipase M from Mucor javanicus in DMSO. Some control experiments were designed to demonstrate the catalytic specificity of lipase. A new strategy for the enzymatic synthesis of drug derivatives was developed by combining aza-Markovnikov addition with acylation procedure involving divinyl esters as linkers. A series of drug derivatives containing N-heterocycles were successfully obtained. The new activity of lipase expands the application of biocatalyst and provides a useful avenue to synthesize drug derivatives.
Two lipase-catalyzed sequential synthesis of drug derivatives in organic media was established based on the new lipase-catalyzed process for aza-Markovnikov addition.Figure optionsDownload as PowerPoint slide
Journal: Enzyme and Microbial Technology - Volume 43, Issues 4–5, 6 October 2008, Pages 375–380