Phenylbutanol derivatives, processes for their preparation and
compositions containing them
    1.
    发明授权
    Phenylbutanol derivatives, processes for their preparation and compositions containing them 失效
    苯乙醇衍生物及其制备方法及其组合物

    公开(公告)号:US4136200A

    公开(公告)日:1979-01-23

    申请号:US810712

    申请日:1977-06-28

    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 1-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.

    Sulfoxides and sulfones
    2.
    发明授权
    Sulfoxides and sulfones 失效
    亚砜和砜

    公开(公告)号:US3981887A

    公开(公告)日:1976-09-21

    申请号:US493459

    申请日:1974-07-31

    CPC分类号: C07D339/08 C07D327/08

    摘要: Sulfoxides and sulfones of the formula ##SPC1##Wherein R.sub.1 is COOH, COOR.sub.4, CH.sub.2 OH, or CH.sub.2 OR.sub.5 ; R.sub.2 is CH.sub.3 or C.sub.2 H.sub.5 ; R.sub.3 is H, F, Cl, or Br; R.sub.4 is alkyl of 1-8 carbon atoms; R.sub.5 is alkanoyl of 2-4 carbon atoms; one of the Y groups is SO or SO.sub.2 and the other Y group is CH.sub.2, O, S, SO, or SO.sub.2 ; and the physiologically acceptable salts thereof, which compounds possess anti-inflammatory activity, can be produced by converting in a compound of the formula ##SPC2##Wherein X is a group convertible into the group --CHR.sub.1 R.sub.2 wherein R.sub.1, R.sub.2, R.sub.3, and Y have the values given above, the group X into the group --CHR.sub.1 R.sub.3.

    摘要翻译: 式WHEREIN R1的亚砜和砜是COOH,COOR4,CH2OH或CH2OR5; R2是CH3或C2H5; R3是H,F,Cl或Br; R4是1-8个碳原子的烷基; R5是2-4个碳原子的烷酰基; Y基团之一是SO或SO 2,另一个Y基团是CH 2,O,S,SO或SO 2; 其化合物具有抗炎活性的生理上可接受的盐可以通过将下式的化合物转化成式WHEREIN X是可转化为基团-CHR1R2的基团,其中R1,R2,R3和Y具有给定值 以上,将X组分组成-CHR1R3。

    Phenylbutanol derivatives and compositions containing them
    6.
    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。