专利号:US-6593347-B2 优先权日:1998-10-30 标题 :Nitrosated and nitrosylated nonsteroidal antiinflammatory compounds, compositions and methods of use 发明人:BANDARAGE UPUL K; DONG QING; FANG XINQIN; GARVEY DAVID S; MERCER GREGORY J; RICHARDSON STEWART K; SCHROEDER JOSEPH D; WANG TIANSHENG 权利人:NITROMED INC 摘要:The present invention describes novel nitrosated and/or nitrosylated nonsteroidal antiinflammatory compounds, and novel compositions comprising at least one nitrosated and/or nitrosylated nonsteroidal antiinflammatory compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase. The present invention also provides methods for treating, preventing and/or reducing inflammation, pain, and fever; decreasing or reversing the gastrointestinal, renal and other toxicities resulting from the use of nonsteroidal antiinflammatory drugs; treating and/or preventing gastrointestinal disorders; treating inflammatory disease states and disorders; and treating and/or preventing ophthalmic diseases or disorders.
专利号:US-10662145-B2 优先权日:2018-08-17 标题:Method of synthesizing diclofenac sodium 发明人:CHEN FENER; WANG LINGDONG; MENG GE; HUANG ZEDU; CHENG DANG; PENG HAIHUI; LIANG GUANFENG 权利人:UNIV FUDAN 摘要:The invention relates to the chemical synthesis of pharmaceutical API, and specifically to a method of synthesizing diclofenac sodium, which is a kind of nonsteroidal anti-inflammatory drug for relieving pain. The method includes: nitrating phenylacetate to prepare o-nitrophenylacetate (2); hydrogenating o-nitrophenylacetate (2) to prepare o-aminophenylacetate (3); amidating an amino group of o-aminophenylacetate (3) to obtain 2-(2-benzoylaminophenyl) acetate (4); 2-(2-benzoylaminophenyl) acetate (4) reacting with thionyl chloride to prepare a chloroimine intermediate, and then condensing the intermediate of chloroimine with 2,6-dichlorophenol using an inorganic base to prepare (E)-methyl-2-(2-((2,6-dichlorophenoxy)(phenyl)methyleneamino) phenyl ester (5); subjecting (E)-methyl-2-(2-((2,6-dichlorophenoxy)(phenyl)methyleneamino) phenyl ester (5) to Chapman rearrangement to afford methyl 2-(2-(N-(2,6-dichlorophenyl)benzoylamino)phenyl) ester (6); and hydrolyzing methyl 2-(2-(N-(2,6-dichlorophenyl)benzoylamino)phenyl) ester (6) to provide the target compound as of diclofenac sodium API. The overall yield is up to 67% based on methyl phenylacetate.
专利号:EG-21151-A 优先权日:1992-07-28 标题:A convenient facile synthesis of 2,6-dichlorod-iphenylamine the key intermediate for the synthesis of 0-(2,6 dichloroanilino) phenylacetic acid diclofenac voltaren) utilizing the firstly reported n- formyl-2,6-dichlorodiphenylamine
专利号:CN-111100057-A 优先权日:2019-12-04 标 题:Synthesis method of diclofenac sodium intermediate 1-(2,6-dichlorophenyl)indoline-2-one
专利号:CN-114539086-B 优先权日:2022-02-25 标题 :Synthesis method of diclofenac sodium
专利号:CN-113429308-A 优先权日:2021-06-16 标题 :The synthesis process of diclofenac sodium
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合成参考文献
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