| 摘要 |
PURPOSE: To obtain a new agent presenting lipoxygenase-inhibitory action and thromboxane synthase-inhibitory action, thus useful for treating or mitigating allergic or inflammatory diseases. CONSTITUTION: This new compound, an N-hydroxyurea compound (or a pharmacologically permissible salt thereof), is expressed by formula I (R is an aryl, the substituted site on the benzene ring being meta or para site), e.g. N- 4-[(2-benzo[b]thienyl-(3-pyridyl)methoxymethyl]benzyl}-N-hydroxyurea of formula II. The compouned of formula II is obtained by the following process: benzo[b]thiophene is reacted with an organometallic reagent to synthesize 2- lithiobenzo[b]thiophene, which is then reacted with pyridine-3-aldehyde to effect conversion into the corresponding alcohol, which is, in turn, reacted with anα-halomethylbenzoic acid ester into the corresponding ester, which is then reduced into the corresponding alcohol, which is, in turn, reacted with N, O-bis(t- butoxycarbonyl)hydroxylamine to effect conversion into the corresponding hydroxylamine, which is finally reacted with trimethylsilyl isocyanate.
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