Water → Linagliptin

Participants

Reaction Conditions

Reaction Steps

Linagliptin-D-(−)-tartrate (45 gm), water (675 mL) and toluene (900 mL) were charged into 5000 mL round bottomed flask and stirred for 10 minutes at 28° C. The resulted solution was heated to 45° C. and 45 mL of 9% aqueous sodium hydroxide solution was added to the mixture at 45° C. (pH is 11.30) and maintained for 1 hour. Layers were separated and organic layer was washed with water (225 mL×2). Combined the organic layers and distilled off the organic layer under vacuum at 45° C. to give 35.4 gm of linagliptin.

Provenance & Evidence