Abstract
A robust and scalable CuI-catalyzed diastereoselective vinylation of an aliphatic aldehyde was developed to enable clinical supply of investigational Mcl-1 inhibitors in our oncology pipeline. Through process design and impurity control, a telescoped process consisting of a benzotriazole salt break and diastereoselective vinylation was developed. This process eliminated the need to perform distillation operations, improved reaction performance and efficiency, and was successfully scaled to >100 kg.
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