4-Hydrazinobenzoic acid → Deferasirox

Participants

Reaction Conditions

Reaction Steps

A suspension of 0.7 g (2.92 mmol) of 2-(2-hydroxyphenyl)benz[e][1,3]oxazin-4-one and 0.52 g (3.44 mmol) of 4-hydrazinobenzoic acid in 8 ml of 2-methyltetrahydrofuran and 5 ml of propionic acid is heated to its boiling point and maintained at this temperature (98° C.) for 2 hours. After completion of the reaction, the mixture is cooled and filtered. The product is washed with 2-methyltetrahydrofuran. After drying, 0.55 g of raw deferasirox is obtained, i.e. 50% of the theory, with an HPLC purity of 95.3% and a melting temperature of 255 to 262° C.

Provenance & Evidence