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Experimental study demonstrates asymmetric hydrogenation of an enamine yielding sitagliptin with high enantiopurity, highlighting an efficient route to synthesize DPP-4 inhibitors.
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 .
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Khopade et al. (2020) studied this question.
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