Jump to main content
Jump to site search
PLANNED MAINTENANCE Close the message box

Scheduled maintenance upgrade on Thursday 4th of May 2017 from 8.00am to 9.00am (BST).

During this time our websites will be offline temporarily. If you have any questions please use the feedback button on this page. We apologise for any inconvenience this might cause and thank you for your patience.


Issue 7, 2012
Previous Article Next Article

Zinc complex mediated regioselective O-acylation of therapeutic agents

Author affiliations

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

Back to tab navigation
Please wait while Download options loads

Supplementary files

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
  •   Request permissions

    Zinc complex mediated regioselective O-acylation of therapeutic agents

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

Search articles by author