Solid-Phase Organic Chemistry: Synthesis of 2β-(Heterocyclylthiomethyl)Penam Derivatives on Solid Support

The impact of combinatorial chemistry of small molecules on the drug discovery process is now widely recognized by the scientific community [1]. Solid-phase organic synthesis (SPOS) is a valuable tool for the generation of structurally diverse compounds for combinatorial libraries. In our work dealing with the solid-phase synthesis of biologically interested compounds, we have developed methodologies for tethering funtionalized polystyrene resins to penicillin derivatives. Our research has also established a new, mild and efficient procedure for the removal of sensitive molecules from Merrifield and Wang resins, using aluminum chloride (AlCl3) [2].