Synthetic Studies towards the Development of Psoralen-Acidic Retinoid Conjugates and Hybrids

Abstract

The chemical modification of trioxsalen using electrophilic aromatic substitution reactions, followed by either Wittig or Heck reactions or Suzuki coupling, allowed for ready access to C4′ modified trioxsalen derivatives that were successfully used for the preparation of a variety of trioxsalen conjugates with acitretin of either the polyamine or the ester type and trioxsalen-acitretin hybrids.

Key words

electrophilic aromatic substitution - Heck reaction - psoralen-retinoid conjugation - Suzuki coupling - Wittig reaction

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