- 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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- 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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- Preparation method of firocoxib
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The invention relates to a preparation method of firocoxib. According to the method, specifically, methylsulfonyl is introduced in the last step of a coupling reaction, and therefore the defect of using thioethers as a starting material (or an intermediate) is avoided.
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- Aryl Methyl Sulfone Construction from Eco-Friendly Inorganic Sulfur Dioxide and Methyl Reagents
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A three-component cross-coupling protocol of boronic acid, sodium metabisulfite, and dimethyl carbonate was developed for the construction of significant functional methyl sulfones, in which introduction of sulfur dioxide at the last stage was successfully achieved in one step. Inorganic sodium metabisulfite was used as an eco-friendly sulfur dioxide source. Green dimethyl carbonate was employed as methyl reagent in this transformation. Diverse functional methyl sulfones were obtained from various readily available boronic acids. Notably, the last-stage modification of pharmaceuticals and the synthesis of Firocoxib were efficiently established through this strategy.
- Wang, Ming,Zhao, Jiaoyan,Jiang, Xuefeng
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p. 3064 - 3068
(2019/02/19)
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- Non-luo kaoxi intermediate preparation method (by machine translation)
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The invention relates to a preparation method of the midbody non-luo kaoxi, belongs to the technical field of pharmacy. The invention provides a preparation method includes: a raw material first after the reaction with the acyl chloride reagent, with in addition a raw material in the presence of a reaction, after treatment, to obtain the target product. The method of the invention can be the operability is strong, is beneficial to the industrial production of operation and cost control. (by machine translation)
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Paragraph 0061; 0062; 0063; 0064; 0065; 0066
(2019/06/08)
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- Synthesis method of Firocoxib
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The invention relates to a synthesis method of Firocoxib. The synthesis method comprises the steps that a compound A serves as a starting raw material to be condensed with acetoxyacetyl chloride to obtain a compound B; ring closing is conducted under the
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Paragraph 0040; 0059-0068
(2018/10/11)
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- Palladium-Catalyzed Thiomethylation via a Three-Component Cross-Coupling Strategy
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In this report, the combination of masked inorganic sulfur and dimethyl carbonate was designed to achieve thiomethylated cross coupling of aryl chlorides. Remarkably, this powerful strategy realized thiomethylation of nucleosides bearing unprotected ribose, chloride-containing pharmaceuticals with late-stage coupling, and herbicides possessing multiple heteroatoms and steric hindrance. Moreover, this protocol is practically amenable to multigram-scale synthesis with a lower catalysis loading and a higher yield.
- Wang, Ming,Qiao, Zongjun,Zhao, Jiaoyan,Jiang, Xuefeng
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p. 6193 - 6197
(2018/09/25)
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- NEW PROCESS FOR THE SYNTHESIS OF FIROCOXIB
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The present invention concerns a process for the preparation of firocoxib, i.e. 3-(cyclopropylmethoxy)-5,5-dimethyl-4-(4-methylsulfonylphenyl)-furan-2-one, comprising steps (a)-(g), wherein the process provides for step (d) of the reaction of a new intermediate, i.e. 2-methyl-1-[4-(methylsulfanyl)phenyl]-1-oxopropan-2-yl (acetyloxy)acetate (compound VII) in the same organic solvent of step (a) in the presence of a catalyst and a phase transfer catalyst solution in the same organic solvent with hydrogen peroxide.
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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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- A PROCESS FOR THE PREPARATION OF FIROCOXIB
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The present invention provides an improved process for preparation of Firocoxib of Formula I. Further, the present invention relates to novel process for the preparation of crystalline polymorphic form B of Firocoxib of Formula I.
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- Firocoxib preparation method
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The invention discloses a firocoxib preparation method and relates to the technical field of chemical synthesis, in particular to a novel method for synthesizing firocoxib. The novel method for synthesizing the firocoxib includes subjecting thioanisole serving as a raw material to acylation reaction, bromination reaction, oxidizing reaction, esterification reaction and cyclization reaction sequentially so as to obtain the firocoxib. Compared with a traditional technology, the novel method for synthesizing the firocoxib has the advantages that an aftertreatment process is simple without column chromatography separation, and the method is high in yield, low in cost and suitable for industrial production.
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- Method of preparing COX-2 inhibitors
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The invention relates to a method for producing compounds of general formula (I) wherein R1 is selected from the following groups: (a) OR5 and (b) mono-, di-, or tri-substituted phenyl; and R2 represents a group (C1-C6) alkyl. The method is characterized
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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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- 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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