Title

Synthesis of thioridazine-VLA-4 antagonist hybrids using N-propargyl northioridazine enantiomers

RIS ID

144377

Publication Details

Martyn, A., Willis, A. & Kelso, M. (2020). Synthesis of thioridazine-VLA-4 antagonist hybrids using N-propargyl northioridazine enantiomers. Synthetic Communications,

Abstract

© 2020, © 2020 Taylor & Francis Group, LLC. Herein, we report the synthesis of thioridazine-VLA-4 hybrid epimers. These hybrid molecules were obtained by means of a click reaction involving N-propargyl northioridazine enantiomers and an azide containing VLA-4 antagonist. A synthesis of northioridazine enantiomers from racemic thioridazine was developed and the absolute stereochemistry was confirmed by X-ray crystallography. Access to N-substituted thioridazine analogs may reveal that this phenothiazine core has therapeutic potential in other disease avenues.

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Link to publisher version (DOI)

http://dx.doi.org/10.1080/00397911.2020.1785503