AZACYCLOALKANE DERIVATIVE AND ABSORBEFACIENT CONTAINING SAID DERIVATIVE AS ACTIVE COMPONENT

NEW MATERIAL:An azacycloalkane derivative of formula I (R is alkyl; m is 2, 3 or 4; n is integer of 1-15; R is 5-11C alkyl when n is 1-3). EXAMPLE:1-(2-Nonylthioethyl)azacyclopentan-2-one. USE:An absorbefacient having remarkable effect to promote the impregnation and permeation of drug in a bio-memb...

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Hauptverfasser: SHIMOZONO YUJI, TSUJI MASAYOSHI, YATANI TERUMI, INOUE TOSHITAKA, KATSUKI MASUMI, NAKAJIMA MIKIO, SAIDA MASARU, SAKAI MICHIYORI
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Sprache:eng
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Zusammenfassung:NEW MATERIAL:An azacycloalkane derivative of formula I (R is alkyl; m is 2, 3 or 4; n is integer of 1-15; R is 5-11C alkyl when n is 1-3). EXAMPLE:1-(2-Nonylthioethyl)azacyclopentan-2-one. USE:An absorbefacient having remarkable effect to promote the impregnation and permeation of drug in a bio-membrane, extremely low topical toxicity and systemic toxicity to bio-membrane and high safety. PREPARATION:The compound of formula I can be produced by reacting a compound of formula IV (n is integer of 2-15) with a compound of formula RSH in a solvent inert to the reaction (e.g. benzene, toluene, etc.) in the presence of a radical polymerization initiator (e.g. benzoyl peroxide, azobisisobutyronitrile, etc.) at 0-150 deg.C for 2-18hr in nitrogen atmosphere or in the absence of the atmosphere.