Novel hydroxyphenylaminobenzenealkanols, useful as antiasthmatic agents, are of the formula
wherein R is hydrogen, lower-alkyl, lower-alkoxy or halo; R'is hydrogen or lower-alkyl; R"is hydrogen, lower-alkyl or halo; and Y is CnH2n wherein n is 1-2. The compounds are prepared by de-etherification of the corresponding phenol alkyl or benzyl ethers; by reduction of the corresponding benzoic acids or esters thereof; or by reduction of ketones wherein -Y-OH is replaced by -COCH3. The invention also relates to the novel benzyl ether intermediates.
可用作抗哮喘药的新型羟苯胺苯烷醇的结构式为
其中 R 是氢、低级烷基、低级烷氧基或卤素;R'是氢或低级烷基;R "是氢、低级烷基或卤素;Y 是 CnH2n,其中 n 是 1-2。这些化合物的制备方法有:相应的苯酚烷基醚或苄基醚的脱醚;相应的苯甲酸或其酯的还原;或酮的还原,其中 -Y-OH 被 -COCH3 取代。本发明还涉及新型苄基醚中间体。
US4496590A
申请人:——
公开号:US4496590A
公开(公告)日:1985-01-29
US4539429A
申请人:——
公开号:US4539429A
公开(公告)日:1985-09-03
Benzyl alcohol derivatives, their preparation and use
申请人:Sterling Drug Inc.
公开号:US04496590A1
公开(公告)日:1985-01-29
Novel hydroxyphenylaminobenzenealkanols, useful as antiasthmatic agents, are of the formula ##STR1## wherein R is hydrogen, lower-alkyl, lower-alkoxy or halo; R' is hydrogen or lower-alkyl; R" is hydrogen, lower-alkyl or halo; and Y is C.sub.n H.sub.2n wherein n is 1-2. The compounds are prepared by de-etherification of the corresponding phenol alkyl or benzyl ethers; by reduction of the corresponding benzoic acids or esters thereof; or by reduction of ketones wherein --Y--OH is replaced by --COCH.sub.3.
Substituted aminophenylalkyl ketones, their preparation and use
申请人:Sterling Drug Inc.
公开号:US04539429A1
公开(公告)日:1985-09-03
Novel lower-alkyl 2-(hydroxyphenylamino)phenyl ketones, useful as inhibitors of lipoxygenase activity, are of the formula ##STR1## wherein R is hydrogen, lower-alkyl, lower-alkoxy or halo; R' is hydrogen or lower-alkyl; R" is hydrogen, lower-alkyl or halo; and Alk is lower-alkyl. The compounds are prepared by de-etherification of the corresponding alkyl or benzyl ethers which are in turn prepared by reacting a 2-(alkoxy- or benzyloxyphenylamino)benzoic acid with an alkyllithium.