- Synthetic method of firocoxib intermediate
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The invention provides a synthetic method of a firocoxib intermediate. The method comprises the steps of carrying out hydroxyl protection, acyl chloride preparation and Friedel-Crafts acylation, and further carrying out a sulfination reaction. The raw materials 2-hydroxy isobutyric acid and bromobenzene are cheap and easily available, and the whole process is concise in step, simple to operate, easy to amplify, high in yield and good in purity. The first three steps adopt a 'one-pot method' reaction, complex post-treatment is not needed, separation and purification are not needed, the next step of reaction is directly carried out, the operation process is greatly simplified, and the production efficiency is improved. In addition, only one solvent is used, the use and recovery of various solvents and the generation of various wastewater and waste gases are avoided, the production cost is greatly reduced, and good industrial application prospects are realized.
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Paragraph 0049; 0057; 0061-0064
(2021/04/10)
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- Preparation method of ferocoxib
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The invention relates to the technical field of medicines, in particular to a preparation method of ferocoxib. According to the preparation method, use of volatile heavy-odor raw material thioanisoleis avoided, and use of volatile high-corrosion heavy-odor isobutyryl chloride is avoided, so that environmental protection advantages are obvious; a hydroxyl compound is used for preparing a compoundwith a structure shown in a formula VI, so that use of liquid bromine with high volatility, high toxicity and high corrosivity can be avoided; a compound with a structure shown in a formula V, acetoxyacetyl chloride, an alkali and an organic solvent are mixed for carrying out an esterification reaction to obtain a compound with a structure shown in a formula VI, so that use of cyclopropoxy aceticacid which cannot be industrially produced on a scale is avoided, and then the process is easier to popularize. A test result shows that the preparation method of ferocoxib is more green and environmentally friendly, is more suitable for industrial popularization, and is far superior to the prior art.
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Paragraph 0086; 0088-0090; 0096; 0098-0100; 0105; 0107-0109
(2019/11/28)
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- Method for preparing firocoxib
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The invention relates to the technical field of medicines and particularly relates to a method for preparing firocoxib. Raw materials used in the preparation method are conventional reagents in the market, thioanisole which is easily volatized and has str
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- Synthetic method for firocoxib important intermediate
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The invention relates to a synthetic method for a firocoxib important intermediate. P-methyl-iso-butyryl benzene is taken as an initial raw material and a one-pot method is adopted for firstly generating a bromide intermediate in a NBS (N-bromosuccinimide
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Paragraph 0044; 0045; 0046; 0047; 0048; 0049-0064
(2019/01/14)
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- Synthesis methods of firocoxib and firocoxib intermediate
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The invention relates to the field of medicine synthesis and provides synthesis methods of firocoxib and a firocoxib intermediate. The synthesis method of the firocoxib intermediate takes 4'-bromopropiophenone as a starting raw material and a condition th
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Paragraph 0098-0108
(2018/03/26)
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- (METHYLSULFONYL)PHENYL-2-(5H)-FURANONES WITH OXYGEN LINK AS COX-2 INHIBITORS
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The invention encompasses the novel compound of Formula (I) useful in the treatment of cyclooxygenase-2 mediated diseases. The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising co
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- Diaryl-2-(5H)-furanones as Cox-2 inhibitors
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The invention encompasses the novel compound of Formula (I) as well as a method of treating cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula (I). The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula (I).
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- ALKYLATED STYRENES AS PRODRUGS TO COX-2 INHIBITORS
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The invention encompasses the novel compound of formula (I) useful in the treatment of cyclooxygenase-2 mediated diseases. The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of formula (I).
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- (methylsulfonyl)phenyl-2-(5H)-furanones with oxygen link as COX-2 inhibitors
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The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising comp
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- (Methylsulfonyl)phenyl-2-(5H)-furanones as COX-2 inhibitors
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The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. STR1 The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.
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- SAR in the alkoxy lactone series: The discovery of DFP, a potent and orally active COX-2 inhibitor
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Extensive SAR has been established in the alkoxy lactone series and this has lead to the discovery of DFP (5,5-dimethyl-3-(2-propoxy)-4- methanesulfonylphenyl)-2(5H)-furanone), a potent COX-2 inhibitor exhibiting in vivo efficacy in all models studied.
- Leblanc,Roy,Boyce,Brideau,Chan,Charleson,Gordon,Grimm,Guay,Leger,Li,Riendeau,Visco,Wang,Webb,Xu,Prasit
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p. 2207 - 2212
(2007/10/03)
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- A new structural variation on the methanesulfonylphenyl class of selective cyclooxygenase-2 inhibitors
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By inserting an oxygen link between the 3-fluorophenyl and the lactone ring of 5,5-dimethyl-3-(3-fluorophenyl)-4-(4-methanesulfonylphenyl)-2(5H)-furanone 1 (DFU), analogs with enhanced in vitro COX-2 inhibitory potency as well as in vivo potency in models of inflammation were obtained.
- Li, Chun-Sing,Black, W. Cameron,Brideau, Christine,Chan, Chi Chung,Charleson, Stella,Cromlish, Wanda A.,Claveau, David,Yves Gauthier, Jacques,Gordon, Robert,Greig, Gillian,Grimm, Erich,Guay, Jocelyne,Lau, Cheuk K.,Riendeau, Denis,Therien, Michel,Visco, Denise M.,Wong, Elizabeth,Xu, Lijing,Prasit, Petpiboon
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p. 3181 - 3186
(2007/10/03)
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- (Methylsulfonyl)phenyl-2-(5H)-furanones as COX-2 inhibitors
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The invention encompasses the novel compound of Formula A that is useful in the treatment of cyclooxygenase-2 mediated diseases. STR1 The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula A.
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- Alkylated styrenes as prodrugs to COX-2 inhibitors
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The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. STR1 The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.
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- 3,4-diaryl-2-hydroxy-2,5-dihydrofurans as prodrugs to COX-2 inhibitors
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The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. STR1 The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.
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