发明名称 Preparation of 4-amino-1-naphthol ether compounds used as pharmaceutical intermediates, by alkylating 1-naphthol, reacting with hydroxylammonium salt and carboxylic acid and hydrolyzing
摘要 Preparation of 4-amino-1-naphthol ether compounds (I) comprises: (a) reacting optionally substituted 1-naphthol compounds (II) with reactive alkyl compounds; (b) reacting the obtained 1-naphthol ether compounds (III) with hydroxylammonium salts and carboxylic acids, and (c) converting the obtained 4-acylamino-1-naphthol ether compounds (IV) into (I) (as free acids or salts) by acidic or basic hydrolysis of the acyl group. An Independent claim is included for new 4-acylamino-1-naphthol ether intermediates of formulae (IV') and (IV''). R1 = 1-12C alkyl, 2-8C haloalkyl, 7-13C aralkyl or A-B; A = 2-8C alkylene or 2-8C haloalkylene; B = NR6R7, SR6 or OR6; R6, R7 = optionally substituted 1-8C alkyl, 1-8C haloalkyl, 7-12C aralkyl or 6-10C aryl, or NR6R7 = 5-8 membered heterocyclyl; R2 = H, halo or 1-4C alkyl; R3 = H, halo, 1-4C alkyl or 1-4C alkoxy; n = 0-4; R4 = halo, NO2, CN, protected formyl, 1-8C alkyl, 7-10C aralkyl, 1-8C hydroxyalkyl, 1-8C haloalkyl, 6-10C aryl or D-E-F'; D = a bond or 1-8C alkylene; E = CO or SO2; F' = R6, OR6, NH2, SR6, NHR6 or NR6R7; R5 = 1-6C alkyl or 1-4C haloalkyl, and X<-> = an anion of an acid.
申请公布号 DE10142461(A1) 申请公布日期 2003.03.20
申请号 DE20011042461 申请日期 2001.08.31
申请人 BAYER AG 发明人 KOMOSCHINSKI, JOACHIM;DIEHL, HERBERT
分类号 C07C213/02;C07C217/94;C07C231/10;C07D295/092;(IPC1-7):C07D295/088;A61K31/537 主分类号 C07C213/02
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