(3)-Azido-methyl-(2,9)-di:oxa-tri:cyclodecane derivs. - with analgesic, antipyretic and antiphlogistic activities

摘要

The dioxatricyclo-decane derivs. of formula (I) are new pharmaceuticals:- In (I) one of R1 and R2 is H, and the other is OH, acyloxy or carbamoyloxy; or together they are oxo. R3 = alkoxy or aralkoxy. The 10,11- double and bond may also be reduced to produce beta-CH3 substit. They are prepd. from the corresp. 3-halomethyl cpd., by reaction with an alkali azide. (I) are already known as intermediates and are now found to have antipyretic, antiphlogistic and analgesic activities. The cpd., 3-azidomethyl-4 beta-acetoxy-8-methoxy-10 beta-methyl-2,9-dioxatricyclo 4,3,1,03,7 decane has intraperitoneal LD50 in mice of 739 mg/kg and has ED50 in the phenylbenzoquinone writhing test of 10 mg/kg orally c.f. 240 mg/kg for acetylsalicyclic acid.