| 摘要 |
<p>1311387 Benzomorphan derivatives SUMITOMO CHEMICAL CO Ltd 19 April 1971 [6 April 1970(2) 10 June 1970] 24212/71 Heading C2C 2-Benzoylalkylbenzomorphan derivatives of the Formula (I) wherein R is H, OH, or C 1-3 alkoxy; R 1 is H, C 1-3 alkyl, phenyl, or phenyl substituted by C 1-3 alkyl, C 1-3 alkoxy, hydroxy, CF 3 , amino, C 1-3 alkythio, nitro, or alkanoyloxy group; R 2 is H or C 1-3 alkyl; R 3 is H, halogen, C 1-3 alkyl, C 1-3 alkoxy, C 1-3 alkylthio, NO 2 , CF 3 , amino or OH group; R 4 is H, C 1-3 alkoxy, halogen, or C 1-3 alkyl; R 5 is H or CH 3 ; and n is an integer of 2 to 4, and salts thereof, all obtained by oxidizing mildly a benzomorphan derivative of Formula (II) The novel compounds of Formula (II) may be obtained by reacting a 2-acyl-benzomorphan derivative of the Formula (III) wherein m is an integer of 1 to 3 and R 6 is H, OH, C 1-3 alkoxy or a group of general formula -OCO(CH 2 ) m CO.C 6 H 3 .(R 3 )(R 4 ), with a reducing agent. The 2-acylbenzomorphan (III) may be obtained by reacting a benzomorphan (IV) with a ketocarboxylic acid (V) or a functionally active derivative thereof. The 2-benzoylalkylbenzomorphans (I) are useful as non-narcotic analgesics, being administered orally or subcutaneously.</p> |
