Improved synthesis of aprepitant, the active ingredient in Emend® — a drug that combats chemotherapy-induced nausea and vomiting. This new process assembles aprepitant in 3 highly atom-economical steps (compared to the traditional 6 steps) and nearly doubles the yield. Compared with the first-generation synthesis, this new route eliminates sodium cyanide, dimethyl titanocene, and gaseous ammonia. This new process also requires only 20% of the raw materials and water used in the original process, eliminating approximately 41,000 gallons of waste per 1,000 pounds of aprepitant. The shorter synthesis process also reduces energy requirements.
Inventor/Owner/Manufacturer/Supplier
Merck & Co., Inc.
Stage of Development
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