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Two lipase-catalyzed sequential synthesis of drug derivatives in organic media

Paper ID Volume ID Publish Year Pages File Format Full-Text
17834 42699 2008 6 PDF Available
Title
Two lipase-catalyzed sequential synthesis of drug derivatives in organic media
Abstract

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.

Graphical abstractTwo 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 full-size imageDownload as PowerPoint slide

Keywords
Promiscuity; Lipase; Aza-Markovnikov addition; N-Heterocycle; Vinyl ester
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Publisher
Database: Elsevier - ScienceDirect
Journal: Enzyme and Microbial Technology - Volume 43, Issues 4–5, 6 October 2008, Pages 375–380
Authors
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Subjects
Physical Sciences and Engineering Chemical Engineering Bioengineering
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Don't Miss Today's Special Offer
Price was $35.95
You save - $31
Price after discount Only $4.95
100% Money Back Guarantee
Full-text PDF Download
Online Support
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