ABSTRACT
The use of opium or alkaloids derived from it, for the purpose of alleviating pain, is about as old as medicine itself. Until 1939 synthetic work on analgesics was mostly limited to derivatives of the opium alkaloids. Out of all of the opium alkaloids, and all of their chemical modifications, morphine remains the most widely used analgesic. Morphine meets all of the narcotic analgesic structure-activity criteria listed in the Introduction. These are the only narcotic analgesics derived from the opium alkaloids which are used in the United States. Modification of another compound in this group of opium alkaloids, oxymorphone, has produced the very valuable naloxone. Work with derivatives of the opium alkaloids was sporadic after 1939, due to the discovery of pethidine. Later, after the morphinans achieved considerable success, most medicinal chemists were occupied with removing as much of the morphine skeleton as possible in the hope of simultaneously removing the side effects of morphine.
