2-cycloalkylmethyl-9,10-dihydroxy-1-(p-...

Details 2-cycloalkylmethyl-9,10-dihydroxy-1-(p-... 2-cycloalkylmethyl-9,10-dihydroxy-1-(p-...

C - Chemistry, Metallurgy

07

D

260/283

C07D 217/24 (2006.01)

Patent

CA 1091675

ABSTRACT OF THE DISCLOSURE N-substituted-14-hydroxy-3-substituted-morphinan derivatives have been found to possess potent narcotic agonist or antagonist activity. In particular, the compound N-cyclo- butylmethyl-3,14-dihydroxymorphian has been found to possess potent agonist/antagonist activity as a non-narcotic analgesic. An improved total synthesis of these compounds is described herein from the starting material 2-(p-methoxybenzyl)-1,2,3,4, 5,6,7,8-octahydroisoquinoline. A preferred feature of the process involves borane reduction of 2-cyclobutylcarbonyl-9,10- dihydroxy-1-(p-methoxybenzyl)perhydroisoquinoline (Va) to provide the corresponding cyclobutylmethyl derivative complexed with borane, which forms the subject matter of this divisional specification. This intermediate is converted directly to N-cyclobutylmethyl-14.beta.-hydroxy-3-methoxymorphinan (LVa) by treating with acid.

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