| 摘要 |
In a process for the prodn. of new methoxybenzene derivs. of formula (I): (where R1 is H or CH3; R2 is 5-8C alkyl or p-Z-phenethyl (Z=H, F or Cl); m is 5 or 6; and Z is COOH or 1H-tetrazol-5-yl), an aldehyde of formula (II) is reacted with a phosphonium salt of the formula Ph3P+-(CH2)m-1X'Y- (III) (where Y is Cl, Br or I) and the prod. is hydrogenated. (I; X'= COOH) may be esterified to give their lower alkyl esters, or converted into acceptable salts by treatment with org. or inorganic bases.(I) have uterine-stimulant and hypotensive activity. (I) have a uterotonic activity in vitro at a concn. of 1-10 mg/l and on the uterus in situ at doses of 40-2000 ug/kg. (I) are partic. suitable for the treatment of essential hypertension, for inducing labour, for eliminating a retained foetus, for terminating pregnancy and for inducing menstruation. Dosage for larger mammals is 10-500 mg/day.Specific cpds. (I) include DL-1-(6-carboxyhexyl)-2-(3-hydroxyoctyl)-4-methoxybenzene. In an example, this is prepd. by reacting 2-(3-hydroxyoctyl)-4-methoxybenzaldehyde with the yield obtd. from 6-carboxyhexyl-triphenylphosphonium bromide and hydrogenating the prod. over Pd/C in glacial acetic acid.
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