Trans-3-Chlor-Acrylnitril置于一水合肼体系中,用 甲醇 用作溶剂,化学反应 4.0H,以60%的收率获得3-氨基吡唑 参考文献:Ege,Guenter; Franz,Hermann,Journal Of Heterocyclic Chemistry,1982,Vol. 19,P. 1267-1273 标题:Ege,Guenter; Franz,Hermann,Journal Of Heterocyclic Chemistry,1982,Vol. 19,P. 1267-1273
专利信息
专利号:US-2009221834-A1 优先权日:2006-04-20 标题 :Synthesis of 5-Beta-Keto-1,2,4-Oxadiazoles and Conversion of 5-Beta-Keto-1,2,4 Oxadiazoles to N-Pyrazolyl Amidoximes 发明人:JENSEN DAVID R; SIDENSTICK JOHN E 权利人:JENSEN DAVID R; SIDENSTICK JOHN E 摘要:The disclosed invention relates to a process for preparing 5-β-keto-1,2,4-oxadiazoles of formula (I), and conversion of 5-β-keto-1,2,4-oxadiazoles (I) into N-pyrazolyl amidoximes of the formula (II) through reaction with hydrazine. The process is defined by two steps. An amidoxime, which may be prepared in situ, is condensed with a β-keto ester to form a 5-β-keto-1,2,4-oxadiazole. The 5-β-keto-1,2,4-oxadiazole is subsequently reacted with hydrazine to furnish the desired N-pyrazolyl amidoxime. The disclosed invention provides several advantages over the current state of the art for the synthesis of N-pyrazolyl amidoximes, which require the condensation of a pyrzolylamine with an actived substrate and subsequent reaction with hydroxyl amine. N-pyrazolyl amidoximes are useful synthetic intermediates, especially for the preparation of photographic developing chemicals.
专利号:US-8076479-B2 优先权日:2006-08-28 标题 :Process and intermediates for the synthesis of (3-alkyl-5-piperidin-1-yl-3,3a-dihydro-pyrazolo[1,5-a]pyrimidin-7-yl)-amino derivatives and intermediates 发明人:CHEN FRANK XING; KEERTIKAR KARTIK M; KUO SHEN-CHUN; LEE HONG-CHANG; RAGHAVAN RAMANI R; WU GEORGE G; XIE JI 权利人:CHEN FRANK XING; KEERTIKAR KARTIK M; KUO SHEN-CHUN; LEE HONG-CHANG; RAGHAVAN RAMANI R; WU GEORGE G; XIE JI; SCHERING CORP 摘要:Disclosed is a process for the synthesis of compounds of Formula I n nby sequentially aminating, first with a primary amine and then with a secondary amine, an intermediate compound of the structure of Formula E1,n n nwherein R 1 is a linear, branched, or cyclic alkyloxy functional group of the structure (—R 2a —OH), R 2a is a linear, branched or cyclic alkyl group, R 2 is a linear, branched or cyclic alkyl group, and R 3 is an alkylene-heterocycle, said process comprising forming intermediate compound of Formula E1 by reacting, in a refluxing reaction solvent selected from alcohols having 5 or less carbon atoms and mixtures of two or more thereof, a methanol solution of a salt of a 4-alkyl-3-amino-pyrazole compound of Formula C1,n n nwith a diamidization reagent selected from dimethylmalonate, monomethylmalonyl-chloride, and malonyl dichloride in the presence of a Lewis base having sufficient proton affinity to abstract a proton from the 1-position nitrogen on the pyrazole ring.
专利号:US-8071782-B2 优先权日:2007-10-02 标 题 :Synthesis of 1,3,4-trisubstituted and 1,3,4,5-tetrasubstituted pyrazoles 发明人:DENG XIAOHU; MANI NEELAKANDHA S 权利人:DENG XIAOHU; MANI NEELAKANDHA S; JANSSEN PHARMACEUTICA NV 摘要:This invention concerns the synthesis of highly substituted pyrazoles, which are structural components of pharmacological compounds, through reaction of hydrazones with nitroolefins.
专利号:US-5719283-A 优先权日:1990-06-20 标 题:Intermediates useful in the synthesis of pyrazolopyrimidinone antianginal agents 发明人:BELL ANDREW SIMON; BROWN DAVID; TERRETT NICHOLAS KENNETH 权利人:PFIZER 摘要:Compounds of the formula ##STR1## wherein R 1 is H, C 1 -C 3 alkyl, C 3 -C 5 cycloalkyl or C 1 -C 3 perfluoroalkyl; n R 2 is H, C 1 -C 6 alkyl optionally substituted by OH, C 1 -C 3 alkoxy or C 3 -C 6 cycloalkyl, or C 1 -C 3 perfluoroalkyl; n R 3 is H, C 1 -C 6 alkyl, C 3 -C 6 alkenyl, C 3 -C 6 alkynyl, C 3 -C 7 cycloalkyl, C 1 -C 6 perfluoroalkyl or (C 3 -C 6 cycloalkyl)C 1 -C 6 alkyl; n and Y is chloro, bromo, or fluoro. n The above compounds are intermediates useful in the synthesis of certain pyrazolopyrimidinones which inhibit cyclic guanosine 3', 5'-monophosphate phosphodiesterase.
专利号:EP-1105359-B1 优先权日:1998-08-21 标 题:Solid phase synthesis of compounds by carbon-carbon bond forming mitsunobu reactions 发明人:CHATURVEDI SURENDRAKUMAR 权利人:PE CORP NY 摘要:Processes are provided for the Mitsunobu alkylation reaction of carbon-carbon bond formation between a solid support reagent and a reagent in solution. The resulting novel products can be prepared as a combinatorial library by high-throughput, parallel synthesis under robotic automation. Cleaved or support-bound products are useful precursors to biologically active compounds.
专利号:US-5679800-A 优先权日:1984-08-30 标题 :2-Amino-3,5,disubstituted-4-halothiophenes and processes for the synthesis thereof 发明人:EGLI ROBERT; HENZI BEAT 权利人:CLARIANT FINANCE BVI LTD 摘要:Compounds of the formula wherein R, R1 and R2 are as defined in the specification and R3 is amino or -N=N-K, wherein K is a coupling component radical. The compounds wherein R3 is -N=N-K are useful as disperse dyes, and those wherein it is amino are useful as intermediates in the synthesis of those wherein it is -N=N-K.
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合成参考文献
摘要:Götzinger, A. C.; Müller, T. J. J., Science of Synthesis Knowledge Updates, (2017) 3, 188. 摘要:Glushkov, V. A.; Shklyaev, Yu. V., Science of Synthesis Knowledge Updates, (2018) 3, 263. 摘要:Xiao, X., Science of Synthesis: Knowledge Updates, (2023) 2, 205. 摘要:Sharma, U.; Parmar, D.; Sumit; Manisha, Science of Synthesis: Knowledge Updates, (2024) 2, 96. 摘要:Hou, W.; Yang, G.; Xu, H., Science of Synthesis: DNA-Encoded Libraries, (2024) nan, 183.