Journal
MOLECULES
Volume 16, Issue 12, Pages 10168-10186Publisher
MDPI
DOI: 10.3390/molecules161210168
Keywords
bile acids; solid-phase synthesis; scaffold decoration; peptidosteroids; convergent ligation
Funding
- Ghent University [BOF 011D16403]
- FWO Vlaanderen [KAN 1.5.186.03, G.0347.04N]
- European Community [MEST-CT-2005-020643]
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We present three versatile solid-supported scaffold building blocks based on the (deoxy) cholic acid framework and decorated with handles for further derivatization by modern ligation techniques such as click chemistry, Staudinger ligation or native chemical ligation. Straightforward procedures are presented for the synthesis and analysis of the steroid constructs. These building blocks offer a new, facile and shorter access route to bile acid-peptide conjugates on solid-phase with emphasis on heterodipodal conjugates with defined spatial arrangements. As such, we provide versatile new synthons to the toolbox for bile acid decoration.
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