| 摘要 |
<p>Methano-benzazocines of formula (I) and their acid addn. salts are new:- In (Ie R is methyl, pentyl, 3-methylbutyl, 2-phenylethyl 2-cyclopropylethyl, 2-cyclobutylethyl or 2-cyclopentylethyl. Prepn. of methano-benzazocines of formula (V) in which one of R2, R'2, R"2 and R'"2 is OH comprises cleaving the alkoxy gp. of a cpd. (V) in which one of R2, R'2, R'"2 is lower alkoxy. In the formula R1 is H, alkyl, alkenyl, alkynyl or haloalkenyl; cycloalkyl, cycloalkyl, alkyl; 2- or 3- furylmethyl (opt. ring substd. by 1-3 methyl or opt. ring-substd. phenyl-alkyl gps., or by 1 or 2 halogen, alkyl, alkoxy, alkanoyloxy or alkylthio, OH CF3 NH2 or alkanoylamino gps. or by one methylenedioxy gp.; one of R2, R'2, R"2, and R'"2 is OH or alkoxy and the others are H, or two adjacent gps. may be methylenedioxy; R3 is H or alkyl. R4 is H, alkyl, alkoxyalkyl, hydroxyalkyl alkylthioalkyl, alkylsulphinylalkyl, phenylthioalkyl, phenyl-sulphinylalkyl, alkenyl or haloalkyl; or R3 and R4 together are (CH2)m (n=3 or 4); R5 is alkylthioalkyl, alkoxyalkyl, lower alkoxy, cycloalkyl cycloalkyl-alkyl or Ar-(CH2)m; Ar is 2- or 3-aryl opt. substd. by 1-3 Me gps. or is phenyl opt. monosubstd. by methylenedioxy or mono- or disubstd. by halogen, alkyl, OH, alkanoyloxy, alkoxy, alkylthio, CF3, NH2 or alkanoylamino gps. m is 0, 2, 3 or 4 all alkyl etc. gps. are lower.</p> |
