| 摘要 |
PURPOSE:To obtain the titled compound which is a nonaddictive compound, orally administrable, and having analgesic effect, by chlorosulfonating benzazocine, reducing the chlorosulfonated benzazocine with a metal and an acid as a reducing agent in the reduction step, and reacting the reduction product with an acyl halide. CONSTITUTION:1,2,3,4,5,6-Hexahydro-2,6-methano-3,6(e), 11(a)-trimethyl-3-benzazocine of formula I is reactaed with chlorosulfonic acid to give a compound of formula II, which is reduced to afford a compound of formula III. The resultant compound of formula III is then reacted with an acyl halide of the formula RCOX (R is alkyl, phenyl or heterocyclic ring; X is halogen) to afford a compound of formula IV. In the reduction step, a metal, e.g. zinc or tin, and an acid, e.g. hydrochloric acid, acetic acid or sulfuric acid, are used as a reducing agent. The above-mentioned catalyst is inexpensive with improved safety.
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