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An efficient synthesis of N-cyclobutylmethylnoroxymorphone from thebaine

โœ Scribed by R.A. Olofson; Joseph P. Pepe

Publisher
Elsevier Science
Year
1977
Tongue
French
Weight
238 KB
Volume
18
Category
Article
ISSN
0040-4039

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โœฆ Synopsis

The search for a safe, effective, and nonaddictive replacement for morphine for the treatment of severe pain has occupied scientists for over a hundred and fifty years. A most promising recent discovery in this area is N-cyclobutylmethylnoroxymorphone (nalbuphine = l), an analgesic now undergoing extensive clinical evaluation. A mixed agonist-antagonist drug, nalbuphine is reported to be as potent an analgesic as morphine and 2-5 times as active a narcotic antagonist as nalorphine.' Similar claims2'3 have been made for other 3,14-dihydroxy-N-cyclobutylmethylmorphinans including the parent compound (butorphanol), ' a highly potent

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