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Scalable Asymmetric Synthesis of MK-8998, a T‑Type Calcium Channel Antagonist

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journal contribution
posted on 28.09.2021, 18:04 by Yong-Li Zhong, Jeffrey C. Moore, Michael Shevlin, C. Scott Shultz, Birgit Kosjek, Yonggang Chen, Jacob M. Janey, Lushi Tan
Two scalable and efficient synthetic routes for the synthesis of a T-type calcium channel antagonist MK-8998 were developed from a simple pyridine building block. The key step to set the stereochemistry relied on either chiral rhodium catalyst-mediated asymmetric hydrogenation of an enamide or transamination of an arylketone that provided the corresponding product in high enantioselectivity and high yield.