509074-26-4Relevant academic research and scientific papers
Preparation method of parecoxib sodium
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Paragraph 0025; 0029; 0033; 0037; 0041; 0045, (2021/04/17)
The invention belongs to the technical field of parecoxib sodium production and provides a preparation method of parecoxib sodium, which comprises the following steps: (1) carrying out sulfonation reaction on acetophenone and chlorosulfonic acid to obtain an intermediate (I) 1-phenyl-2-(4-sulfonyl chloride phenyl)acetophenone; (2) carrying out acetylation reaction on the intermediate I and acetyl chloride to obtain an intermediate (II) 1-phenyl-2-(4-sulfonyl chloride phenyl)-2-acetyl ethanone; (3) refining the intermediate II; (4) carrying out cyclization reaction on the refined intermediate II and hydroxylamine hydrochloride to obtain an intermediate III 4-(5-methyl-3-phenyl-4-isoxazole)benzenesulfonyl chloride; (5) carrying out ammoniation reaction on the intermediate III and ammonia water to obtain an intermediate IV 4-(5-methyl-3-phenyl-4-isoxazole)benzenesulfonamide; (6) carrying out propionylation reaction on the intermediate IV and propionic anhydride to obtain parecoxib; and (7) carrying out salt forming reaction on the intermediate V and sodium hydroxide to obtain the parecoxib sodium. The technical problems that an existing parecoxib sodium synthesis method is complex in reaction process and high in production cost are solved.
Parecoxib sodium genetic toxicity impurity and preparation method of same
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Paragraph 0052; 0074-0077; 0095-0098; 0110-0113; 0125-0140, (2020/04/17)
The invention relates to a parecoxib sodium genetic toxicity impurity and a preparation method of same. The preparation method includes: at -5 to 0 DEG C, mixing 5-methyl-3,4-diphenyl isoazole and dichloromethane and adding chlorosulfonic acid at the rate
Preparation method of parecoxib sodium
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Paragraph 0038-0045, (2020/05/14)
The invention belongs to the technical field of medicines, and particularly relates to a preparation method of parecoxib sodium. 5-methyl-3, 4-diphenyl isoxazole is used as a raw material, and the parecoxib sodium is obtained through sulfonation reaction, ammoniation reaction, propionylation reaction and salification. The method has the advantages of mild reaction, easy operation, great reductionof the generation of HCl gas, short reaction time, high product yield, and suitableness for industrial production.
Synthesis method of parecoxib sodium impurities
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Paragraph 0008; 0022, (2020/11/10)
The invention discloses a synthesis method of a parecoxib sodium impurity N-ethyl-5-[4-(5-methyl-3-phenyl-4-isoxazolyl) phenyl] sulfonamide, 5-methyl-3, 4-diphenyl isoxazole is used as a raw material,the parecoxib sodium impurity is obtained through sulfo
Handkerchief auspicious past cloth sodium impurities and its preparation method
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Paragraph 0027; 0028; 0029; 0030, (2019/05/22)
The invention provides a handkerchief auspicious past cloth sodium impurities and its preparation method, the impurity is 4, 4' - (sulfonyl (4, 1 phenylene)) b (5 - methyl - 3 - phenyl isoxazole). The present invention provides a compound can be used as a
A handkerchief auspicious past cloth sodium freeze-dried powder, its preparation method and its powder products
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Paragraph 0054; 0055; 0056, (2019/06/11)
The invention discloses a parecoxib sodium freeze-dried powder, a preparation method and a powder product thereof. The freeze-dried powder comprises 95-100 wt% of the parecoxib sodium and 0-5 wt% of a pH regulator; or 40-100 wt% of the parecoxib sodium and 0-60 wt% of L-malate. The freeze-dried powder has simple preparation method, is free of auxiliary materials or employs few auxiliary materials, is reduced in cost, and satisfies national medicine standards in storage stability, clinical application stability and safety.
Bone-targeted parecoxib sodium nanocapsule freeze-dried injection and preparation method thereof
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Paragraph 0031-0033, (2017/10/25)
The invention discloses a bone-targeted nanocapsule freeze-dried injection containing parecoxib sodium and a preparation method of the injection. By virtue of a preparation, namely the injection, the concentration of parecoxib sodium in a bone tissue can be increased, so that the effects of parecoxib sodium in orthopedic surgeries and bone cancer analgesia are improved. By utilizing a capsule material and a carrier material which have good biodegradability and biocompatibility, a drug can be tightly combined with soft and hard tissues in a human body in a short time after entering the human body so as to rapidly play a role of treatment. By utilizing a nanocapsule packaging manner, the content of degradation products of the preparation is extremely low.
Preparation method of parecoxib sodium synthesis technology impurities
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Paragraph 0038; 0045, (2016/10/31)
The present invention provides a preparation method of parecoxib sodium synthesis technology impurities. The method comprises the step of using 5-methyl-3,4-diphenylisoxazole as a raw material to synthesize a target product 4-(5-methyl-3-phenyl-isoxazolyl
Application of [3+2]-cycloaddition in the synthesis of valdecoxib
Reddy, Anumula Raghupathi,Goverdhan, Gilla,Sampath, Aalla,Mukkanti, Khagga,Reddy, Padi Pratap,Bandichhor, Rakeshwar
, p. 639 - 649 (2012/01/13)
A large scale synthesis of valdecoxib 1 is described. Our work features potential application of [3+2]-dipolar cycloaddition involving enamine and in situ-generated nitrile oxide derivatives. Dr. Reddy's Laboratories Ltd.
Chemical and biological investigation of N-hydroxy-valdecoxib: An active metabolite of valdecoxib
Erdelyi, Peter,Fodor, Tamas,Varga, Agnes Kis,Czugler, Matyas,Gere, Aniko,Fischer, Janos
, p. 5322 - 5330 (2008/12/22)
The inhibition of cyclooxygenase enzymes plays an important role in the treatment of inflammatory diseases. N-Hydroxy-4-(5-methyl-3-phenylisoxazol-4-yl)benzenesulfonamide (3)-a primary metabolite of the highly selective COX-2 inhibitor valdecoxib-was synthesized and stabilized as its monohydrate (3a·H2O). The anti-inflammatory properties of 3a·H2O were investigated in carrageenan-induced edema and in acute and chronic pain models. Based on our biological investigation, we conclude that N-hydroxy-valdecoxib 3a is an active metabolite of valdecoxib.
