Isopropyl Acetate → Erlotinib Hydrochloride

Participants

Reaction Conditions

Reaction Steps

Erlotinib free base (10 gm) is added to isopropyl acetate (400 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. and stirred for 2 hours 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 the mixture of isopropyl acetate (40 ml) and ethyl acetate (4 ml) and then dried at 50-55° C. to give 9.9 gm of erlotinib hydrochloride crystalline polymorph form A having polymorph form B undetected [HPLC Purity: 99.89%; to Moisture Content: 0.15%; Mean particle size (D50): 5.48 μm and 90 volume-% of the particles (D90): 18.96 μm].

Provenance & Evidence