Trifluoroacetic acid → Bisegliptin

Participants

Reaction Steps

Using (2S,4S)-1-[2-[(4-ethoxycarbonylbicyclo[2.2.2]oct-1-yl)amino]acetyl]-4-fluoropyrrolidine-2-carboxamide (3.70 g), trichloroacetic anhydride (1.9 mL) as a dehydrating agent and trifluoroacetic acid (0.78 mL) as an acid, a white powder of (2S,4S)-1-[2-[(4-ethoxycarbonylbicyclo[2.2.2]oct-1-yl)amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile was obtained (obtained amount: 2.86 g, yield: 81%) by the same method of Example 1.

Provenance & Evidence