PYROCATECHOL DERIVATIVE AND 5-LIPOXYGENASE ACTION INHIBITOR CONTAINING SAME AS ACTIVE CONSTITUENT

摘要

NEW MATERIAL:A pyrocatechol derivative of formula I (Y is lower alkoxyl, piperidyl, pyrrolidyl or formula II or III). EXAMPLE:N-5-(3,4-Dihydroxyphenyl)-2,4-pentadienoylpiperidine. USE:Medicines, having the inhibitory action on 5-lipoxygenase, and effective for allergic asthma, allergic rhinitis, etc. PREPARATION:A compound of formula IV (R' is methoxyethoxymethyl group or dimethyl-tert-butylsilyl group) is reacted with a compound of formula V (R is ethyl or propyl) in the presence of sodium hydride (NaH) to give a compound of formula VI. The dimethyl-tert-butylsilyl group in the compound of formula VI is eliminated with tetrabutylammonium fluoride, and the methoxyethoxymethyl group is treated with P-toluenesulfonic acid to afford the compound of formula I (Y is ethoxy or propoxy group).