Abstract Octahydro-1 H-benzofuro [3, 2-e] isoquinolines, which possess the ACNO partial structure of morphine, displayed potent oral analgesic and narcotic-antagonism activity. However, due to inefficiency in their synthesis the ACNO derivatives have not been developed for clinical use. Here, we report in detail the first asymmetric total synthesis of (-)- octahydro-1 H-benzofuro [3, 2-e] isoquinoline as exemplified by the preparation of (-)-1 ...
