This talk will be presented as an overview of various methodologies and platform developments that have occurred over the 15 years I have spent at Merck & Co. The first half of the talk will feature the utilization and development of various Negishi reagents. These reagents have been applied toward the synthesis of novel BACE inhibitors via a one-pot sp3/sp2 Negishi couplings. Moreover, the developmet and expansion of bench-stable Negishi reagents that can be employed in parallel synthesis to evolve structure-activity-relationships (SAR) of small molecules and their biological targets will also be discussed. More recent developments in the area of creating novel reagents for converting pharmacologically relevant small molecules into tools to perform mechanism-of-action (MOA) elucidation studies will also be discussed. More specifically, optimization of the chemistry for diazirine-containing reagents that can be employed in photocrosslinking experiments. Preliminary results from photoaffinity labeling will be shared as well.

Developing methodologies and reagents to enable drug discovery and identify novel molecular targets

256th National Meeting (2018)

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