Low-epimerization amide coupling conditions have been developed using T3P (n-propanephosphonic acid anhydride) for the synthesis of a key intermediate to a hepatoselective glucokinase activator. These conditions were incorporated into a process involving very easy reaction setup and product isolation. Subsequent debenzylation via transfer hydrogenation at ambient pressure provides API with excellent purity and throughput.

Scalable amide bond formation and transfer hydrogenation for the synthesis of a hepatoselective glucokinase activator

243rd National Meeting (2012)

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