专利号:US-11040938-B2 优先权日:2016-07-27 标 题 :Continuous flow process for the synthesis of phenylhydrazine salts and substituted phenylhydrazine salts 发明人:MA BING; PAN SHUAI 权利人:SHANGHAI HYBRID—CHEM TECH; SHANGHAI HYBRID CHEM TECH 摘要:The present invention provided a continuous flow process for the synthesis of phenylhydrazine salts and substituted phenylhydrazine salts. Diazotization, reduction, acidic hydrolysis and salifying with acids are innovatively integrated together. Using acidic liquids of aniline or substituted aniline, diazotization reagents, reductants and acids as raw materials, phenylhydrazine derivative salts is obtained through the synthesis process, which is a three-step continuous tandem reaction including diazotization, reduction, acidic hydrolysis and salifying. The described synthesis process is a kind of integrated solutions, which is carried out in an integrated reactor. The feed inlets of the integrated reactor are continuously filled with raw materials. In the integrated reactor, diazotization, reduction, acidic hydrolysis and salifying are carried out continuously and orderly, and phenylhydrazine salts or substituted phenylhydrazine salts is obtained in the outlet of the integrated reactor without interruption. The total reaction time is no more than 20 min.
专利号:US-6025492-A 优先权日:1996-08-30 标 题 :Synthesis of a hydrazone β-keto ester by the reaction with a diazo ester 发明人:SHAH AJIT S; CLARK JERRY D; MA YINONG; PETERSON JAMES C; PATELIS LEFTERIS 权利人:MONSANTO CO 摘要:The present invention relates to the synthesis of a hydrazone β-keto ester by the reaction of an alkyl diazoester with a hydrazone aldehyde in the presence of a Lewis acid In a preferred embodiment, the hydrazone β-keto ester is then converted into a pyridazinone compound by the reaction with an alkyl acid chloride in the presence of a base, followed by acidification. A process for the production of a hydrazone aldehyde, which comprises contacting a hydrazine and glyoxal, is also described.
专利号:US-7153960-B2 优先权日:2001-12-10 标 题:Synthesis of 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones 发明人:ZHOU JIACHENG; OH LYNETTE M; MA PHILIP; LI HUI-YIN; CONFALONE PASQUALE 权利人:BRISTOL MYERS SQUIBB CO 摘要:A novel process and intermediates thereof for making 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones of the type shown below from appropriate phenyl hydrazines is described. n nThese compounds are useful as factor Xa inhibitors.
专利号:US-7442802-B2 优先权日:2002-06-27 标 题:Cyclooxygenase-2 selective inhibitors, compositions and methods of use 发明人:BANDARAGE UPUL K; EARL RICHARD A; EZAWA MAIKO; FANG XINQIN; GARVEY DAVID S; KHANAPURE SUBHASH P; RANATUNGE RAMANI R; RICHARDSON STEWART K; SCHROEDER JOSEPH D; STEVENSON CHERI A; WEY SHIOW-JYI 权利人:NITROMED INC 摘要:The invention describes novel cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one COX-2 selective inhibitor, optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor, and/or, optionally, at least one therapeutic agent. The novel cyclooxygenase 2 selective inhibitors of the invention can be optionally nitrosated and/or nitrosylated. The invention also provides methods for treating inflammation, pain and fever; for treating and/or improving the gastrointestinal properties of COX-2 selective inhibitors; for facilitating wound healing; for treating and/or preventing renal and/or respiratory toxicity; for treating and/or preventing other disorders resulting from elevated levels of cyclooxygenase-2; and for improving the cardiovascular profile of COX-2 selective inhibitors.
专利号:US-3651226-A 优先权日:1970-03-18 标题 :Miticidal compositions containing phenylazopropenoate esters and methods of use 发明人:STICKER ROBERT EARL 权利人:FMC CORP 摘要:A NEW CLASS OF MITICIDES COMPRISES PHENYLAZOPROPENOATE ESTERS OF THE FORMULA (R''-OOC-C(-R')=C(-R)-N=N-),(X)N,(Y)M-BENZENE WHEREIN R IS HYDROGEN OR AN ALIPHATIC GROUP HAVING ONE TO THREE CARBON ATOMS INCLUSIVE; R' IS HYDROGEN OR METHYL; R'' IS A LOWER ALIPHATIC HYDROCARBON GROUP, SATURATED OR UNSATURATED, OR LOWER ALKOXYALKYL; X IS HALOGEN, LOWER ALKYL, LOWER ALKOXY, OR LOWER ALKYLTHIO; Y IS METHYL OR CHLORO; N IS 0 OR 1; AND M IS 0, 1, OR 2. SYNTHESIS OF MANY OF THIS CLASS OF COMPOUNDS, THEIR PHYSICAL PROPERTIES, AND THEIR EFFECTIVENESS AGAINST MITES AND MITE EGGS ARE DESCRIBED.
专利号:US-6297194-B1 优先权日:1999-02-02 标 题 :Production of phosphonopyrazoles 发明人:MILLER PAULA C; CURTIS JANE M; MOLYNEAUX JOHN M; OWEN THOMAS J 权利人:MONSANTO TECHNOLOGY LLC 摘要:Pyrazole compounds with activity as chemical hybridizing agents and methods for synthesis of such compounds are disclosed. These compounds are useful in producing hybrid wheat (Triticum aesativum) and other crops.
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合成参考文献
参考文献:10.1007/s00706-012-0849-7 摘要:Sławiński J, Żołnowska B, Orlewska C, Chojnacki J. Synthesis and molecular structure of novel 2-(alkylthio)-4-chloro-N-(4,5-dihydro-5-oxo-1H-1,2,4-triazol-3-yl)-5-methylbenzenesulfonamides with potential anticancer activity. Monatshefte für Chemie - Chemical Monthly. 2012 Sep 25;143(12):1705–18. doi: 10.1007/s00706-012-0849-7. 参考文献:10.1007/s11030-020-10045-x 摘要:Kostopoulou I, Diassakou A, Kavetsou E, Kritsi E, Zoumpoulakis P, Pontiki E, Hadjipavlou-Litina D, Detsi A. Novel quinolinone-pyrazoline hybrids: synthesis and evaluation of antioxidant and lipoxygenase inhibitory activity. Mol Divers. 2021 May;25(2):723–40. doi: 10.1007/s11030-020-10045-x.