Methanesulfonic Acid → Erlotinib Hydrochloride

Participants

Reaction Conditions

Reaction Steps

5 g of 4-chloro-6,7-bis(2-methoxyethoxy) quinazoline was suspended in 150 ml denatured spirit (SPDS) and 4.6 g of 3-aminophenyl acetylene was charged at 25-30° C. Further 1.0 ml of methane sulphonic acid was added. The reaction mass was stirred at 25-30° C. for 3 hours. Solid obtained was filtered, washed with SPDS and dried under vacuum. This solid was suspended in water, basified with ammonia and stirred for 10 minutes. The resulting erlotinib base was isolated, washed with water and dried under vacuum. The base was suspended in water and acidified to pH 1.0-2.0 using hydrochloric acid. The reaction mixture was stirred for 2 hours, filtered, washed with water and dried at 40-45° C. to obtain 5.8 g of erlotinib hydrochloride.

Provenance & Evidence