Small, nitrogen-containing heterocycles, particularly isoquinolines and derivatives thereof, are privileged scaffolds represented across many approved therapeutics, natural products, and drug-discovery campaigns. Thus, new methods for their synthesis are continuously being sought after by the scientific community. One active area of research that we have exploited utilizes transition-metal catalyzed C-H activation as an atom economic strategy to construct new carbon-carbon bonds. This presentation will focus on the synthesis of a diverse set of medicinally relevant isoquinoline motifs and derivatives thereof employing readily available coupling partners in annulation reactions with carboxylic acid derivatives.

Rhodium-catalyzed C-H activation to construct isoquinoline derivatives

ACS Spring Meeting 2021

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