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Issue 7, 2012
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Zinc complex mediated regioselective O-acylation of therapeutic agents

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Abstract

Several Zn β-diiminate reagents were developed and used to mediate regioselective O-acylation reactions of therapeutic agents with anhydrides. Various prodrugs were obtained in excellent yield and high regioselectivity, including derivatives of rapamycin and paclitaxel. Furthermore, the application of regioselective acylation was extended to one-pot reactions between therapeutics and carboxylic acids with various pendant functional groups. This rapid functionalization strategy will find application in either prodrug synthesis or bioconjugation for drug delivery.

Graphical abstract: Zinc complex mediated regioselective O-acylation of therapeutic agents

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Publication details

The article was received on 25 Feb 2012, accepted on 06 Apr 2012 and first published on 11 Apr 2012


Article type: Edge Article
DOI: 10.1039/C2SC20239E
Citation: Chem. Sci., 2012,3, 2234-2239
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    Zinc complex mediated regioselective O-acylation of therapeutic agents

    R. Tong and J. Cheng, Chem. Sci., 2012, 3, 2234
    DOI: 10.1039/C2SC20239E

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