90536-66-6Relevant articles and documents
Preparation method of etoricoxib intermediate 4-methylsulphonyl phenylacetic acid
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Paragraph 0032; 0033, (2018/03/26)
The invention belongs to the technical field of medicines, and discloses a preparation method of etoricoxib intermediate 4-methylsulphonyl phenylacetic acid. The method comprises the following steps:taking 4-methylsulfonyl acetophenone as an initial raw material, using fluoboric acid (HBF4.SiO2) supported on silica gel as the catalyst to synthesize 2-(4-(methylsulfonyl) phenyl)-1-morpholinoethanethione, hydrolyzing the 2-(4-(methylsulfonyl) phenyl)-1-morpholinoethanethione to obtain the etoricoxib intermediate 4-methylsulphonyl phenylacetic acid. The preparation method does not need toxicityreagents in other synthetic routes; the use of the fluoboric acid supported on silica gel as the catalyst conquers the defects of the traditional Willgerodt-Kindler reaction such as high temperature,long time and low yield, and moreover the method is simple to operate and easy to control and suitable for industrial production.
FUSED THIOPHENE AND THIAZOLE DERIVATIVES AS ROR GAMMA MODULATORS
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Page/Page column 33; 35; 37, (2015/07/16)
The present invention provides fused thiophene and thiazole derivatives of formula (I), which may be therapeutically useful, more particularly as RORγ modulators; in which R1, R2, R3, R4, R5, R6, R7, X1, X2, L, m, n and ring A have the meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention of diseases or disorders, in particular their use in disease(s) or disorder(s) where there is an advantage in modulating RORγ receptor. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the fused thiophene and thiazole derivatives of formula (I), together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
TRISUBSTITUTED HETEROCYCLIC DERIVATIVES AS ROR GAMMA MODULATORS
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Page/Page column 32; 34, (2014/09/03)
The present invention provides trisubstituted heterocyclic derivatives of formula (I), which may be therapeutically useful, more particularly as RORγ modulators; (I) in which R1, R2, R3, Ra, X, L, m and ring A have the meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention of diseases or disorder, in particular their use in diseases or disorder where there is an advantage in modulating RORγ receptor. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the trisubstituted heterocyclic derivatives of formula (I) together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
