| 摘要 |
NEW MATERIAL:An azacycloalkane derivative expressed by formula I (R is alkyl; m is 2-4; n is 2-15). EXAMPLE:1-(6-Pentyloxycyclohexyl)azacyclopentan-2-one. USE:Capable of being blended with an absorption accelerator useful for the pharmaceutical industry or cosmetics, e.g. quasi-drugs, etc., and agricultural chemicals, insecticides, etc., having improved enhancing action on penetrability and permeability of drugs into biomembranes, e.g. skin, mucosa, etc., and further individual antimicrobial action and high safety with very weak local irritancy to the biomembranes and systemic toxicity, etc. PREPARATION:For example, a compound expressed by formula IV is reacted in the presence of an alkali catalyst, etc., to form a compound expressed by formula II (M is alkali metal ion), which is then reacted with a compound expressed by formula V (X is halogen, mesyl, etc.) to afford a compound expressed by formula III. The resultant compound expressed by formula III is further reacted with an alcohol expressed by the formula R-OH in the presence of an alkali catalyst to give the aimed compound expressed by formula I.
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