| 摘要 |
<p>4-benzyloxy-piperidine derivs. and their acid addition salts have formula (I) are novel. In (I) a) R is ethoxycarbonyl and R1, R2, R3 are 3-methyl, 3-trifluoromethyl, 4-chloro 2,4-dichloro or 2-naphthylmethoxy; b) R is methyl and R1, R2, R3 are 3, 4, 5-trimethoxy, 4-chloro, 3-trifluoromethyl or 3,4-dichloro; c) R is benzyl and R1, R2, R3 are 3, 4, 5-trimethoxy, 3,4-dichloro or 4-chloro; d) R is H and R1, R2, R3 are 4-chloro, 3,4-dichloro, 4-isopropyloxy, 4-isopropyl, 2-naphthylmethoxy or 4-bromo e) R is 2-hydroxy-ethyl and R1, R2, R3 are 3,4-dichloro or 2,4-dichloro; f) R is 4-chlorobenzyl, 2-chlorobenzyl, phenethyl or 3-chlorobenzyl and R1, R2, R3 are 3, 4, 5-trimethoxy; g) R is phenethyl, 4-methoxy-benzyl, 4, 3 or 2-chlorobenzyl or 3-phenyl-propyl and R1, R2, R3 are 4-methoxy; h) R is 3-phenylpropyl and R1, R2, R3 are 4-chloro and i) R is methoxycarbonyl and R1, R2, R3 are 3,4-dichloro. Prepn. comprises (b) reacting (II) and (III) b) Opt. removal or reduction of protecting gp. c) (I) (R is H) may be reacted with R-Z. In the formulae (where R1 is a N-protecting gp., such as 4-nitrobenzoyl, opt. substd. benzoyl, opt. substd. benzyl or alkyl and Y is a reactive gp., such as Cl or Br and Z is a reactive gp.) Antidepressants, which may be administered orally or parenterally in daily doses of 5-200 mg. Reserpine antagonism and 5-hydroxy-tryptophane, head-twitching activity tests are described. The LD50 1.p in mice varies from 30-1000mg/kg.</p> |
