ABSTRACT

The interface between medicinal chemistry and process research groups is critical to the rapid evaluation and development of new clinical candidates. The discovery of drug molecules is often followed with structural optimization for potency and selectivity by diverse and thorough structure-activity-relationship studies. These studies rely upon versatile and general synthetic techniques and strategies that are often not the most pragmatic approaches to specific congeners. As a result, the biological activity of a family of molecules can be investigated in a timely fashion to reveal the most potent drug substance with the least side effects. Notwithstanding, the resulting chemical synthesis that allowed the initial construction of the drug candidate is frequently inappropriate for scale-up beyond several milligrams of material. The design of a synthesis for a general class of compounds, therefore, rarely considers the same criteria as that for a specific target compound.