Optical resolution of (+/-)-2,5-dimethyl-2'-hydroxy-9alpha- and -9beta-propyl-6,7-benzomorphans and their pharmacological properties

J Med Chem. 1976 Mar;19(3):430-2. doi: 10.1021/jm00225a021.

Abstract

The levo and dextro isomers of 2,5-dimethyl-2'-hydroxy-9alpha- and -9beta-propyl-6,7-benzomorphans have been prepared. The analgesic potency and physical dependence capacity of the optical isomers and their racemic parents were determined. The 9alpha-propyl levo isomer was analgesically equipotent with morphine; the 9beta-propyl levo isomer was considerably more potent subcutaneously and equipotent orally. None of the optical isomers suppressed the withdrawal syndrome; the 9beta-propyl levo isomer exacerbated the withdrawal syndrome.

MeSH terms

  • Analgesics / chemical synthesis
  • Animals
  • Benzomorphans / analogs & derivatives
  • Benzomorphans / chemical synthesis*
  • Benzomorphans / pharmacology
  • Haplorhini
  • Humans
  • Mice
  • Morphinans / chemical synthesis*
  • Morphine Dependence / physiopathology
  • Optical Rotation
  • Stereoisomerism
  • Substance-Related Disorders / etiology

Substances

  • Analgesics
  • Benzomorphans
  • Morphinans