Hydrochloric Acid → Erlotinib Hydrochloride

Participants

Reaction Conditions

Reaction Steps

Crude erlotinib free base (10 gm, HPLC purity: 98.2%; Content of N-methoxyethyl impurity: 0.24%) is dissolved in dimethylsulfoxide (50 ml) at 25-30° C., to the solution is added 15% methanolic HCl (100 ml) at 25-30° C. while the pH of the mass is adjusted to 2 and then stirred for 30-40 minutes at 25-30° C. The material is filtered, washed with a mixture of dimethyl sulfoxide (10 ml) and methanol (20 ml), and then the material is dried at 60-65° C. under vacuum for 5 hours to give 8.9 gm of pure erlotinib hydrochloride [HPLC purity: 99.92%; Content of N-methoxyethyl impurity: 0.02% (at 1.14 RRT)].

Provenance & Evidence