Dimethyl Sulfoxide → Sunitinib Malate

Participants

Reaction Steps

Sunitinib free base (5.0 gm), L-malic acid (1.8 gm) and dimethyl sulfoxide (25 ml) are mixed and the mixture was heated to 80 deg C. to obtain a clear solution, stirred for 30 minutes at 80 deg C. The solution was slowly cooled to room temperature and the solution was added to methyl tert-butyl ether (150 ml), stirred for 15 hours at room temperature. The solid obtained by filtration and the solid was washed with mixture of dimethyl sulfoxide (1 ml) and methyl tert-butyl ether (9 ml), and then dried at 60 deg C. under vacuum to obtain 4 gm of sunitinib malate crystal form I.

Provenance & Evidence