The Diels-Alder-Reaction With Inverse-Electron-Demand - A Review Of An Efficient & Attractive Click-Reaction Concept

INTERNATIONAL JOURNAL OF PHARMACEUTICAL SCIENCES AND RESEARCH(2013)

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摘要
Here, we review the development of prospective image processing systems in molecular diagnostics and of pharmacologically active ingredients for patient-specific therapeutic approaches. These projects require not only high demands on quality, safety, and specificity but also, rapid, efficient and irreversible ligation routes during the synthesis of future pharmaceuticals. The Diels-Alder ligation reaction with inverse electron demand (DAR(inv)) is an eligible technology not restricted to medical applications, but valuable in selective modification by functionalization of polymers, organic and inorganic surfaces and micro arrays. Additionally, the DARinv technology is considered as an attractive strategy-platform for efficient syntheses of promising pharmacologically active components and derivatives of natural molecules with an optimized therapeutic index. We like to encourage scientists working with the brilliant concept of Sharpless. s "Click chemistry", to intensify their research with this valuable DARinv technology able to open the door for regioselective, stereospecific, and bioorthogonal exigent syntheses of substances of highest quality inconceivable so far.
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关键词
Bioorthogonal, Click-Chemistry, Ligation chemistry, inverse Diels Alder Reaction, Regioselectivity & Stereospecificity, Therapy & Diagnostics
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