Tetrahydrofuran → Afatinib dimaleate

Participants

Reaction Steps

THF (0.5 ml) was added to 200 mg (0.41 mmol) afatinib free base and the mixture was stirred at room temperature to obtain a light yellow coloured solution. A solution of 100 mg (0.8 mmol) maleic acid in 0.5 ml THF was added over the course of 2 min. Another 4 ml THF were added and the mixture was stirred for 1 h. The solids were filtered off, rinsed with 2 ml THF and dried on a rotary evaporator at 48° C./3 mbar for 6 h to give 0.245 g (83% yield) of a white solid.

Provenance & Evidence