New acylation reagent improves drug syntheses

Scientists in the US have developed an acylation reagent that can address shortcomings in the acylation of several complex natural products and therapeutics that are widely used in disease treatment and clinical trials. 

The reactions include the inefficient regioselective acylation in rapamycin and paclitaxel and the inefficient acylation of tertiary hydroxyl groups in camptothecin.

c2sc20239e-ga

 

Link to journal article
Zinc Complex Mediated Regioselective O-Acylation of Therapeutic Agents
R Tong and J Cheng
Chem. Sci., 2012, DOI: 10.1039/c2sc20239e

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