New neurokinin (NK-1) receptor antagonist crystal form and preparation method thereof

Abstract

The invention provides a new neurokinin (NK-1) receptor antagonist aprepitant crystal form V. The new aprepitant crystal form V powder has characteristic X diffraction ray peaks at the wavelengths of 12.08 degrees + / -0.2, 15.31 degrees + / -0.2, 17.61 degrees + / -0.2, 20.62 degrees + / -0.2 and 24.76 degrees + / -0.2 2 theta in an X-ray diffraction pattern. The invention also provides a preparation method of the aprepitant new crystal form V.

Description

technical field [0001] The invention belongs to the field of medicine and chemical industry, and in particular relates to a new crystal form V of aprepitant, a neurokinin (NK-1) receptor antagonist, and a preparation method thereof. Background technique [0002] Aprepitant (aprepitant), the chemical name is 5-[2(R)-[1(R)-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3(S)- (4-fluorophenyl)morpholin-4-ylmethyl]-3,4-dihydro-2H-1,2,4-triazol-3-one, the structure is as follows: [0003] [0004] Aprepitant is a neurokinin-1 (NK-1) receptor antagonist developed by Merck & Co of the United States. It was approved by the FDA in 2003, and its trade name is Emend. This product is clinically used as a tablet to prevent acute and delayed nausea and vomiting caused by highly emetogenic anti-tumor chemotherapy drugs (including high-dose cisplatin therapy), which can pass through the blood-brain barrier and communicate with the brain NK-1 receptors selectively bind to play an antiemetic eff...

AI Technical Summary

Problems solved by technology

This product is clinically used as a tablet to prevent acute and delayed nausea and vomiting caused by highly emetogenic anti-tumor chemotherapy drugs (including high-dose cisplatin therapy), which can pass through the blood-brain barrier and communicate with the brain Selective binding of NK-1 receptors exerts antiemetic effects, but has little affinity for 5-HT3, dopamine and glucocorticoid receptors

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