Design and Development of Pd‐Catalyzed Aerobic N‐Demethylation Strategies for the Synthesis of Noroxymorphone in Continuous Flow Mode

• Published in: European journal of organic chemistry Vol. 2017; no. 4; pp. 914 - 927
• Main Authors: Gutmann, Bernhard, Cantillo, David, Weigl, Ulrich, Cox, D. Phillip, Kappe, C. Oliver
• Format: Journal Article
• Language: English
• Published: WEINHEIM Wiley 26.01.2017; Wiley Subscription Services, Inc
• Subjects: Chemistry; Chemistry, Organic; Demethylation; Flow chemistry; Microreactors; Opioid antagonists; Oxygen; Palladium; Physical Sciences; Science & Technology; Sythesis design; Oxygen; MORPHINE; Flow chemistry; TERTIARY-AMINES; NALOXONE; Sythesis design; Palladium; Opioid antagonists; Demethylation; THEBAINE; OXYMORPHONE; NALTREXONE; Microreactors; SOLIDS; CHEMISTRY; TOOL

Strategies for the generation of noroxymorphone from 14‐hydroxymorphinone are presented. Noroxymorphone is the key intermediate in the synthesis of various opioid antagonists, including naloxone, naltrexone, and nalmefene, as well as mixed agonists‐antagonists such as nalbuphine. The transformation...