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The method of obtaining derivatives of biphenyl or their salts, or racemates, or optically active antipodes

机译:获得联苯衍生物或其盐,外消旋物或旋光对映体的衍生物的方法

摘要

1411495 3 - (Fluoro - 4 - biphenylyl) - 3- hydroxy - butyric acids and derivatives thereof DR KARL THOMAE GmbH 16 Aug 1973 [17 Aug 1972] 38843/73 Heading C2C The invention comprises compounds of the formula wherein R 1 is F in the 21- or 4SP1/SP-position, B is OH, alkoxy or a group in which R 2 and R 3 are H, -CH 2 COOH, (C 1 -C 5 )alkyl or phenyl optionally substituted by OH or CH 3 , and where B is OH, the salts of thereof with inorganic or organic bases. Compounds in which B is alkoxy may be obtained by reacting a compound of the formula with the Zn compound of an appropriate haloacetate ester in the presence of an organic solvent. Compounds in which B is OH and salts thereof may be obtained by saponification of compounds of Formula I in which B is alkoxy with an alkali or a strong acid and liberating the free acids from salts thereof by acidification with a mineral acid. Compounds in which B is may be obtained by reacting compounds of Formula I in which B is alkoxy or compounds in which said alkoxy group is replaced by a halogen atom, with an amine of the formula Examples are given for the production of the compounds. The compounds of Formula I have antiphlogistic activity and may be administered orally, rectally or parenterally in conventional forms.
机译:1411495 3-(氟-4-联苯基)-3-羟基丁酸及其衍生物DR KARL THOMAE GmbH 1973年8月16日[1972年8月17日]标题C2C本发明包括下式的化合物,其中R 1为F在21或4 1 位,B为OH,烷氧基或R 2和R 3为H,-CH 2 COOH,(C 1 -C 5)烷基或苯基的基团被OH或CH 3取代,且其中B为OH时,其与无机或有机碱形成的盐。 B为烷氧基的化合物可通过在有机溶剂存在下使式的化合物与适当的卤代乙酸酯的Zn化合物反应而获得。 B为OH的化合物及其盐可以通过用碱或强酸将其中B为烷氧基的式I化合物皂化并通过用无机酸酸化而从其盐中释放游离酸来获得。可以通过使其中B为烷氧基的式I化合物或其中所述烷氧基被卤素原子取代的化合物与下式的胺反应来获得其中B的化合物。实施例给出了化合物的制备。式I化合物具有抗炎活性,可以常规形式口服,直肠或肠胃外给药。

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