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Atropisomerism in drug candidates can create synthetic and regulatory challenges. Molecules that exist as stable atropisomers can be acceptable for development but can still be difficult to synthesize in pure form. With the withdrawal of lesinurad, Amgen’s sotorasib is the only remaining fully-synthetic drug marketed as a stable atropisomer.

Now, modern catalytic methods have greatly expanded access to molecules exhibiting atropisomerism, and many interesting drug candidates that exist as stable atropisomers are in development.

In this article, the team at Sinocompound highlights examples of development candidates that exist as stable atropisomers, synthetic routes used to access them, and a particularly interesting kilo-scale synthesis of a Ph. III candidate using asymmetric catalysis.

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Sinocompound is a global provider of advanced homogeneous catalysts and ligands and specialist services for a range of pharmaceutical and fine chemical applications. We have expertise ranging from R&D all the way through to scale-up and commercial manufacturing. Our proven process is built around our next generation technologies, flexibility, and speed-of-response ensuring delivery at the scale required for your project. Our success is due to our dedication to listening to customers and developing bespoke solutions that help the industry overcome its challenges and customers accelerate their route to market. In order to facilitate this process further, we also offer catalyst screening and custom synthesis services.


Find out how to scale your product when limited by catalyst availability here.
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