The synthesis of some bridgehead N,O-heterocycles of biological interest.
The preparation of 5-aryl-6-oxa-1-azabicyclo[3,3,0]octanes, 6-aryl-5-oxa-1-azabicyclo[4,3,0]nonanes and 7-aryl-6-oxa-1-azabicyclo[5,3,0]decanes from the corresponding substituted omega-chlorobutyrophenones and aminoalcohols is described; and the ring opening reactions are studied. A preliminary biologic activity study has also been conducted, and demonstrated that the 5-(2,5-dimethyl)phenyl-6-oxa-1-azabicyclo[3,3,0]octane possesses antiinflammatory activity.
D000700:Analgesics / Q000138:chemical synthesis; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis; D055598:Chemical Phenomena; D002621:Chemistry; D005260:Female; D006571:Heterocyclic Compounds / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D007928:Lethal Dose 50; D008722:Methods; D051381:Rats
D000700:Analgesics; D000893:Anti-Inflammatory Agents; D006571:Heterocyclic Compounds