Aprepitant Intermediate
This compound (CAS 200000-59-5), chemically (2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)morpholine 4-methylbenzenesulfonate, is an advanced chiral intermediate in the manufacture of the antiemetic drug aprepitant. It is a solid that should be stored dry, cool and protected from light and moisture, and it is catalogued as a pharmaceutical intermediate rather than a finished active substance. The molecule carries several defined stereocentres and two trifluoromethyl groups that confer high lipophilicity and metabolic stability, while the tosylate salt provides crystallinity, purity control and enantiopurity assurance. As a late-stage intermediate it already contains the fully assembled morpholine core and the fluorinated aromatic substituents of the final active pharmaceutical ingredient, so only a small number of further steps remain to reach the finished drug substance.
1. Antiemetic drug synthesis: a key chiral intermediate in the production of aprepitant, a neurokinin-1 receptor antagonist used to prevent chemotherapy-induced nausea and vomiting and postoperative nausea, and in the related drug fosaprepitant.
2. Trifluoromethyl chemistry value: demonstrates how the 3,5-bis(trifluoromethyl)phenyl group raises potency, lipophilicity and metabolic stability, a motif now widely exploited in modern drug design, process chemistry and analogue optimisation.
3. Analytical and regulatory importance: controlled as a defined process intermediate with specifications for stereochemical purity, related substances, residual solvents and metal content in drug master file documentation, batch records and regulatory submissions.
4. Handling and storage: keep sealed in a cool, dry place away from light and oxidising agents; use protective equipment to avoid dust inhalation, and note that the tosylate counter-ion is a potential alkylating species requiring controlled waste handling and disposal.
Product Name: Aprepitant Intermediate
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