PRODUCTION OF AZACYCLOALKANE DERIVATIVE
PURPOSE:To obtain the subject high-purity compounds useful in the fields of medical and agricultural chemicals in a high yield with economic advantage by carrying out a radical reaction between an azacycloalkan-2-one and an alkylmercaptane and subsequently treating the reaction product with a reduci...
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Zusammenfassung: | PURPOSE:To obtain the subject high-purity compounds useful in the fields of medical and agricultural chemicals in a high yield with economic advantage by carrying out a radical reaction between an azacycloalkan-2-one and an alkylmercaptane and subsequently treating the reaction product with a reducing agent. CONSTITUTION:A 1-(n-alkenyl)azacycloalkan-2-one of formula I (m is 1-3; n1 is 0-8) is reacted with an alkylmercaptane in the presence of a radical initiator (e.g. benzoyl peroxide) in a solvent such as ethanol at 50-150 deg.C. The resultant reaction product it then treated with a reducing agent (e.g. tributylphosphine) in a water-containing organic solvent (e.g. ethanol) at 0-100 deg.C followed by distillation and purification, thus obtaining the objective compound of formula II (R is 3-12C alkyl). The obtained compound of formula II can improve penetrability and permeability of a drug and is useful as an absorption promoter low in irritation to the biomembranes and low in systematic toxicity. |
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