Phenylbutanol derivatives and compositions containing them
    36.
    发明授权
    Phenylbutanol derivatives and compositions containing them 失效
    苯基丁醇衍生物和含有它们的组合物

    公开(公告)号:US4049823A

    公开(公告)日:1977-09-20

    申请号:US552959

    申请日:1975-02-25

    摘要: Phenylbutanol derivatives of the formula Z--C(CH.sub.3) (OH)--CH.sub.2 --Y wherein Z is 4-biphenyl or 4-phenoxyphenyl wherein the phenoxy group is unsubstituted or substituted by F, Cl or Br and Y is COOR.sup.2 or CH.sub.2 OR.sup.3 wherein R.sup.2 is H or alkyl of 1 to 6 carbon atoms and R.sup.3 is H or alkanoyl of 1 to 6 carbon atoms, and their physiologically acceptable salts, possess anti-inflammatory activity and are produced by (a) treating with a solvolyzing agent a compound of the formula Z--C(CH.sub.3) (OH)--CH.sub.2 --W or Z--CX(CH.sub.3)--CH.sub.2 --Y wherein W is a functionally modified carboxy or methylol group different from Y and X is Cl, Br or I or a functionally modified hydroxyl group; or (b) reducing a compound otherwise corresponding to a desired final product but having instead of one of the hydrogen atoms a group which can be reduced or replaced by a hydrogen atom; or (c) oxidizing a compound otherwise corresponding to a desired final product but lacking the tertiary hydroxyl group; or (d) converting a compound otherwise corresponding to a desired final product wherein Z is a 4-phenoxyphenyl group but having instead a 4--OH--, Cl--, Br-- or I-substituted phenyl group into a desired final product; or (e) diazotizing a compound otherwise corresponding to a desired final product wherein Z is a halogen-substituted 4-phenoxyphenyl group but having an --NH.sub.2 -substituted phenoxy group and reacting the resulting diazonium salt with a halogenating agent.

    摘要翻译: 式ZC(CH3)(OH)-CH2-Y的苯基丁醇衍生物,其中Z为4-联苯基或4-苯氧基苯基,其中苯氧基未被取代或被F,Cl或Br取代,Y为COOR2或CH2OR3,其中R2为H 或1〜6个碳原子的烷基,R 3为H或1〜6个碳原子的烷酰基,其生理学上可接受的盐具有抗炎活性,并通过(a)用溶剂分解剂处理式ZC化合物 (CH 3)(OH)-CH 2 -W或Z-CX(CH 3)-CH 2 -Y,其中W是不同于Y的官能改性羧基或羟甲基,X是Cl,Br或I或官能改性羟基; 或者(b)还原与所需最终产物相对应的化合物,但是其中一个氢原子可以被氢原子还原或取代的基团取代; 或(c)氧化其它对应于所需最终产物但不含叔羟基的化合物; 或(d)将其它对应于所需最终产物的化合物转化成所需的最终产物,其中Z是4-苯氧基苯基,但代之以4-OH-,Cl-,Br-或I-取代的苯基转化成所需的最终产物; 或(e)重氮化其它对应于所需最终产物的化合物,其中Z是卤素取代的4-苯氧基苯基但具有-NH 2取代的苯氧基,并使所得重氮盐与卤化剂反应。