Simultaneous release of two therapeutic reagents, mertansine and CO through photo-induced cleavage of a mitochondria-specific prodrug with improved drug efficacy.
A highly enantioselective synthesis of sitagliptin, a potent DPP‐4 inhibitor, is reported. Explicitly identified chiral FerroLANE ligands in the presence of rhodium catalyze the asymmetric hydrogenation of an enamine to yield sitagliptin with excellent enantioselectivity (98% ee). The process was scaled up to 5 g and the final product was isolated as a phosphate salt with >99% ee.
Diabetes is on the rise across the Globe and millions of people are being affected. Sitagliptin has emerged as a potent inhibitor for the treatment of type II diabetes, which can regulate blood sugar level, and new strategies to prepare this molecule are being discovered. Herein we report a highly enantioselective synthesis of sitagliptin. Using specifically identified chiral FerroLANE ligands in the presence of a rhodium catalyst the asymmetric hydrogenation of an enamine to yield sitagliptin with excellent enantioselectivity (98% ee). The final product has been isolated as a phosphate salt with >99% ee. More information can be found in the Full Paper by Samir Chikkali et al. on page 189 in Issue 2, 2020 (DOI: 10.1002/ajoc.201900709).
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