Fumaric Acid → Tenofovir Disoproxil Fumarate

Participants

Reaction Conditions

Reaction Steps

Tenofovir disoproxil (25 kg) was dissolved in isopropyl alcohol (100 liters) at 25-30° C. Fumaric acid (10 kg) was added and the mixture was heated to 50-55° C. for 1 hour, gradually cooled to 25-30° C., further chilled to 10° C. and stirred for 4 hours. The resulting solid was filtered and washed with chilled isopropyl alcohol. The wet cake was stirred in isopropyl acetate (200 ltrs.) at 10-15° C. for 4 hours. The solid was filtered and washed with chilled isopropyl acetate and dried under vacuum to obtain 30 kg of tenofovir disoproxil fumarate.

Provenance & Evidence