Class 3 Atropisomers In Focus: Custom Manufacturing To Capture Therapeutic Selectivity In Oncology

Once considered a minor challenge, atropisomerism is now a critical focus in small molecule drug manufacturing. These axially chiral molecules, resulting from restricted rotation around a single bond, can have one isomer that is significantly more biologically active than the other. With approximately 30% of all FDA-approved drugs displaying atropisomerism, isolating the highly active isomer is essential for enhancing efficacy and specificity while minimizing unwanted off-target effects.

Developing stable, single-isomer atropisomers presents a complex but crucial opportunity for scalable drug production. Learn about an effective, three-fold manufacturing strategy that addresses this challenge: utilizing robust Suzuki couplings for constructing the biaryl structures common to atropisomers; achieving high-efficiency isomer separation using Simulated Moving Bed (SMB) chromatography; and integrating continuous flow racemization of the undesired isomer with SMB separation for maximized yield.

Discover how advanced technologies are making the manufacture of single-isomer atropisomers scalable from clinic to commerce. Understand how these strategies are being applied in modern small molecule drug development.