Hydrochloric Acid → Erlotinib Hydrochloride

Participants

Reaction Steps

Into a 3 Lt. four necked round-bottomed flask provided with a mechanical stirrer, thermometer socket, reflux condenser etc., are charged 2400 mL of methylene chloride, followed by 120 g of Erlotinib base (Prepared according to the process given in Example-(1) of PCT International Publication No. WO 2007/060691) under stirring. The reaction mass is slightly warmed up to 37±1° C., so that the Erlotinib base completely dissolves in the solvent. Then carbon treatment is given and the filtrate is transferred to 5 Lt. three necked round bottomed flask, provided with a mechanical stirrer and other accessories. To this filtrate, isopronolic HCl (HCl content as 100% is 13.90 g) is added in one lot at 30-35° C. and then the reaction mass is refluxed for about 3 hrs. Afterwards, the reaction mass is cooled to room temperature and filtered. The product is washed with methylene chloride and the wet cake is dried to get 119 g of Erlotinib hydrochloride as a white crystalline powder.

Provenance & Evidence