Journal
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
Volume 56, Issue 36, Pages 10924-10927Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201706367
Keywords
alkynylation; C-H activation; drug conjugation; palladium; peptides
Categories
Funding
- Scripps Research Institute
- NIH (NIGMS) [2R01GM084019]
- Bristol-Myers Squibb
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The palladium(II)-catalyzed C(sp(3))-H alkynylation of oligopeptides was developed with tetrabutylammonium acetate as a key additive. Through molecular design, the acetylene motif served as a linchpin to introduce a broad range of carbonyl-containing pharmacophores onto oligopeptides, thus providing a chemical tool for the synthesis and modification of novel oligopeptide-pharmacophore conjugates by C-H functionalization. Dipeptide conjugates with coprostanol and estradiol were synthesized by this method for potential application in targeted drug delivery to tumor cells with overexpressed nuclear hormone receptors.
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