Diethyl Ether → Erlotinib Hydrochloride

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Reaction Steps

Erlotinib free base (5 gm, obtained in reference example 3) is dissolved in chloroform (200 ml) at 25-30° C. to form a clear solution and then added diethyl ether (50 ml). To the resulting solution slowly added 15% diethyl ether HCl (5 ml) at 25-30° C. and stirred for 30 minutes at 25-30° C. Filtered the material, washed with a mixture of diethyl ether (10 ml) and chloroform (10 ml), and then dried at 60-65° C. under vacuum to give 4.9 gm of erlotinib hydrochloride polymorph form A [HPLC purity: 99.7%; Mean particle size (D50): 3.50 μm and 90 volume-% of the particles (D90): 4.61 μm].

Provenance & Evidence