Hydrochloric Acid → Erlotinib Hydrochloride

Participants

Reaction Conditions

Reaction Steps

115 g (0.292 mol) of erlotinib base was added to 2300 ml (20 vol) of 1-pentanol at 25-30° C. The mixture was cooled to 5 to 10° C. and stirred for 30 min. to obtain a suspension. 57.5 g of aqueous hydrochloric acid at a concentration of 35% (w/w) was added drop wise at 5-10° C. and the mixture stirred for 1 hour. The product was isolated by filtration and washed with 230 ml (2 vol.) of 1-pentanol. The product was dried under reduced pressure (50 mm Hg) at 0-60° C. to obtain 113 g of erlotinib hydrochloride polymorph A as a white solid.

Provenance & Evidence