Dataset Information
Palladium(II)-Catalyzed Site-Selective C(sp3 )-H Alkynylation of Oligopeptides: A Linchpin Approach for Oligopeptide-Drug Conjugation.
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ABSTRACT:
SUBMITTER: Liu T
PROVIDER: S-EPMC5572133 | biostudies-literature | 2017 Aug
REPOSITORIES: biostudies-literature
Publications
Palladium(II)-Catalyzed Site-Selective C(sp<sup>3</sup> )-H Alkynylation of Oligopeptides: A Linchpin Approach for Oligopeptide-Drug Conjugation.
Angewandte Chemie (International ed. in English) 20170807 36
The palladium(II)-catalyzed C(sp<sup>3</sup> )-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 synthesi ...[more]