Chemical reduction of naltrexone is described in an attempt to synthesize 6β‐hydroxynaltrexone. Only the epimer, 6α‐hydroxynaltrexone, was produced. Pilot metabolic studies on naltrexone in the dog, rat, and guinea pig were made to determine which animal produced the greatest amount of 6β‐hydroxynaltrexone. The guinea pig was selected and used to produce the metabolite. Isolation and purification methods are described, and spectral data are presented for structural confirmation of the metabolite.
- 6α‐Hydroxynaltrexone—synthesis via chemical reduction of naltrexone
- 6β‐Hydroxynaltrexone—isolation and identification as naltrexone metabolite in guinea pig
- Naltrexone—chemical reduction to 6α‐hydroxynaltrexone, metabolism in dog, rat, and guinea pig
ASJC Scopus subject areas
- Pharmaceutical Science