Osimertinib ketorolac salt crystal form and preparation method thereof

Abstract

The invention belongs to the technical field of medicines, and particularly relates to an osimertinib ketorolac salt crystal form and a preparation method thereof. An X-ray diffraction pattern expressed by 2theta and utilizing Cu-Kalpha radiation, of the crystal form, has characteristic peaks at 4.9+ / -0.2 degrees, 6.4+ / -0.2 degrees, 12.2+ / -0.2 degrees, 21.+ / -0.2 degrees and 22.6+ / -0.2 degrees. Theosimertinib ketorolac crystal form is low in hygroscopicity, simple in preparation process, stable in property and suitable for large-scale production.

Description

technical field

[0001] The invention belongs to the technical field of medicine, and in particular relates to a crystal form of osimertinib ketorolate and a preparation method thereof. Background technique

[0002] If lung cancer patients have EGFR or ALK gene mutations, the use of targeted drugs can obtain better survival benefits. However, the effects of these drugs are generally short-lived, with resistance developing within 9-11 months, which occurs because cancer cells are able to evade treatment with EGFR or ALK inhibitors by mutating and changing the way they grow active.

[0003] Osimertinib, developed by AstraZeneca, is a third-generation oral, irreversible, selective EGFR mutation inhibitor that can be used for both activating and resistant mutant EGFR, that is, for patients with advanced non-small cell lung cancer, 50% of acquired resistance to anti-EGFR therapy is caused by the T790M mutation, and osimertinib can render this challenging mutation ineffective. O...

Images