Microwave-Assisted Solid-Phase Organic Synthesis (MA-SPOS) of Oxazolidinone Antimicrobials

Microwave-assisted solid-phase organic synthesis (MA-SPOS) is a valuable methodology for the rapid synthesis of novel and diverse chemical entities. The recent advances in microwave equipment have provided homogeneous microwave heating in safe and reliable instruments for use in the chemistry laboratory. A MA-SPOS of the antimicrobial oxazolidinone pharmacophore is described in this chapter as a demonstration of the utility of this emerging technology towards drug discovery. The optimization process and full experimental details for the synthesis of a small library of oxazolidinones are exemplified. The oxazolidinones comprise a unique class of potent antibacterial agents. MA-SPOS enables the combinatorial chemist to break through the solid-phase synthetic chemistry optimization bottleneck and develop new reaction conditions in hours or days rather than weeks or months. The rapid production of the libraries of novel compounds has thus, been enabled by synergizing the best aspects of MA chemistry and SPOS.