Erlotinib → Erlotinib Hydrochloride

Participants

Reaction Conditions

Reaction Steps

Erlotinib free base (10 gm) is added to methyl isobutyl ketone (300 ml) under stirring at 25-30° C., the contents are heated to 60° C. and then stirred at 60-65° C. to form a clear solution. To the solution slowly added 7% ethyl acetate HCl (40 ml) at 60-65° C., the resulting mass is slowly cooled to 25-30° C. and then stirred for 1 hour. Filtered the mass, washed with methyl isobutyl ketone (20 ml) and then dried at 50-55° C. to give 9.8 gm of erlotinib hydrochloride crystalline polymorph form A having polymorph form B undetected (HPLC Purity: 99.87%, Moisture Content: 0.2%).

Provenance & Evidence