Timely progression of hit-to-lead chemical matter in small molecule drug discovery programs depends heavily upon realizing the chemical synthesis of designed analogs. Inevitably, the complexity of synthetic targets increases as medicinal chemistry projects mature and advance toward clinical candidate nomination. In order to avoid “the road not taken,” strategic investment in the development of novel methods for the preparation of key synthetic intermediates and for functionalization of late-stage compounds can aid greatly in project advancement. This presentation will detail some of the author’s efforts in the Discovery Chemistry department at Genentech, Inc. to develop new synthetic methods to enable rapid structure-activity relationship (SAR) studies in several drug discovery campaigns. With an emphasis on leveraging Genentech’s undergraduate summer intern program, the deployment of both transition metal-catalyzed C-H functionalizations as well as photoredox-nickel dual-catalyzed strategies will be discussed.

Catalytic transition metal and photoredox methods development to enable medicinal chemistry SAR exploration

ACS Spring Meeting 2021

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