Hydrochloric Acid → Erlotinib Hydrochloride

Participants

Reaction Steps

10.0 g crystal form IV of erlotinib base was added to 200 ml 1,4-dioxane, heated to dissolve until being clarified, 6.4 g isopropanol saturated with HCl gas was added dropwise at 60-70° C., after dripping, stirred for 30 minutes while maintaining the temperature, stirred for 1 hour at 0-15° C. before filtration, dried at 50° C. to obtain 10.6 g sample of crystal form A. The yield was 97.2% and the purity was 99.8% (by HPLC).

Provenance & Evidence