Francis Gosselin

Synthesis of the pan-TEAD Inhibitor GDC-8025 via a Flow Chan–Evans–Lam Coupling and Enantioselective Biocatalytic α-Ketoester Reduction

Abstract GDC-8025 is a potent pan-TEAD inhibitor that features a functionalized 1H-pyrazolo[3,4-b]pyridine core and a reactive acrylamide warhead. The first-generation synthesis of GDC-8025 relied on a Sharpless asymmetric dihydroxylation of 7 to install the chiral diol moiety (8...

Data-driven construction of an imine reductase library capable of broad-scope reductive amination at equimolar substrate concentrations

Reductive amination catalysed by imine reductases and reductive aminases has emerged as a powerful method for the asymmetric synthesis of chiral amines, yet the generality and practical limitations of these enzymes remain poorly understood. Here, we combine large-scale, iterative...