氟乙酰胺置于盐酸体系中,化学反应生成 氟乙酸乙酯 参考文献:Bacon Et Al.,Journal Of The American Chemical Society,1948,Vol. 70,P. 2654 标题:Bacon Et Al.,Journal Of The American Chemical Society,1948,Vol. 70,P. 2654
专利号:US-5204478-A 优先权日:1992-08-20 标题 :Process for the synthesis of 2,6-dichloro-5-fluoronicotinic acid and 2,6-dichloro-5-fluoronicotinoyl chloride 发明人:JENNINGS REX A 权利人:WARNER LAMBERT CO 摘要:An improved process for the preparation of 2,6-dichloro-5-fluoronicotinoyl chloride is described where a 2,6-dihydroxy-5-fluoronicotinic acid ester is converted in one step using phosphorus oxychloride and a lithium reagent to 2,6-dichloro-5-fluoronicotinoyl chloride and subsequent basic hydrolysis affords 2,6-dichloro-5-fluoronicotinic acid.
专利号:US-6121448-A 优先权日:1995-03-28 标题 :Pyrimidine compounds 发明人:LEWIS ROBERT ANDREWS; GOODBY JOHN WILLIAM; TOYNE KENNETH JOHNSON; HIRD MICHAEL 权利人:SECR DEFENCE BRIT 摘要:The synthesis of novel compound (I) is described: 5-bromo-2-iodopyrimidine may be used for the synthesis of a range of chemical compounds both known and novel. The synthesis of a number of novel liquid crystalline compounds is described.
专利号:WO-2025124470-A1 优先权日:2023-12-15 标 题:Doravirine intermediate, and use thereof and synthesis method therefor 发明人:GAO ZHANGBIN; WEN SHAOPENG; YANG JINHONG; JU JINGJING; MAO WENXIU 权利人:SHANDONG CHENGCHUANG BLUE SEA PHARMACEUTICAL TECH CO LTD 摘要:The present invention relates to a doravirine intermediate, and the use thereof and a synthesis method therefor, which belong to the technical field of pharmaceutical chemistry. The method for synthesizing the doravirine intermediate comprises the following steps: (1) mixing ethyl 2-fluoroacetate with 4-ethoxy-1,1,1-trifluoro-3-buten-2-one with solvent I, and then dropwise adding sodium bis(trimethylsilyl)amide to form compound 1; (2) adding an ammonia source into the reaction liquid of compound 1 to obtain compound 2; (3) dissolving compound 2 in solvent II, adding a catalyst, and heating and ring-closing the mixture to obtain compound 3; and (4) dissolving compound 3 in toluene, adding thionyl chloride, and dropwise adding pyridine to obtain 2-hydroxy-3-fluoro-4-trifluoromethylpyridine. The synthesis method of the present invention has a low raw material cost and a short process period, is environmentally friendly, and is suitable for process scaled-up production.
专利号:WO-2021031168-A1 优先权日:2019-08-21 标 题:Continuous synthesis method for 2-fluoromalonic acid diester compound 发明人:HONG HAO; LU JIANGPING; BAO DENGHUI; LIU CHAOJIE; CAI XUEDONG; JIA XIAOTONG 权利人:ASYMCHEM LIFE SCIENCE TIANJIN CO LTD 摘要:Provided is a continuous synthesis method for a 2-fluoromalonic acid diester compound. The method comprises: using (I) as a raw material, and carrying out continuous decarbonylation reaction in a continuous reaction device to obtain 2-fluoromalonic acid diester compound (II), wherein R and R' respectively represent unbranched or branched alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclic or cyclic alkyl, and R and R' are the same or different. Compared with the traditional kettle reaction, the amount of materials involved in the reaction per unit time is decreased and the high-temperature dangerous area is reduced in the synthesis method, thereby greatly lowering the safety risk.
专利号:US-7179906-B2 优先权日:1996-04-01 标 题 :Asymmetric benzoxanthene dyes 发明人:BENSON SCOTT C; MENCHEN STEVEN M; THEISEN PETER D; HENNESSEY KEVIN M; FURNISS VERGINE C; HAUSER JOAN D 权利人:APPLERA CORP 摘要:A class of asymmetric monobenzoxanthene compounds useful as fluorescent dyes are disclosed having the structure n nwherein Y 1 and Y 2 are individually hydroxyl, amino, imminium, or oxygen, R 1 –R 8 are hydrogen, fluorine, chlorine, alkyl, alkene, alkyne, sulfonate, amino, amido, nitrile, alkoxy, linking group, and combinations thereof, and R 9 is acetylene, alkane, alkene, cyano, substituted phenyl, and combinations thereof. The invention further includes novel intermediate compounds useful for the synthesis of asymmetric benzoxanthene compounds having the general structuren n nwhere substituents R 3 –R 7 correspond to like-referenced substituents in the structure of described above, and Y 2 is hydroxyl or amine. In another aspect, the invention includes methods for synthesizing the above dye compounds and intermediates. In yet another aspect, the present invention includes reagents labeled with the asymmetric benzoxanthene dye compounds, including deoxynucleotides, dideoxynucleotides, phosphoramidites, and polynucleotides. In an additional aspect, the invention includes methods utilizing such dye compounds and reagents including dideoxy polynucleotide sequencing and fragment analysis methods.
专利号:US-3682917-A 优先权日:1970-03-25 标题 :Method for producing 5-fluorouracil 发明人:KNUNIANTS IVAN LJUDVIGOVICH; GERMAN LEV SOLOMONOVICH; KAZMINA NATALIA BORISOVNA 权利人:IVAN LJUDVIGOVICH KNUNIANTS; LEV SOLOMONOVICH GERMAN; NATALIA BORISOVNA KAZMINA 摘要:The present invention concerns the method for producing 5fluorouracil. In accordance with the said method uracil is brought to interact with fluorine in diluent medium which partly or completely dissolves uracil without interacting with fluorine, in an atmosphere of inert gas with subsequent separation of the formed end product. It is preferable to employ acetic acid as diluent, and nitrogen as the inert gas. The end product 5fluorouracil finds wide application in cancer therapy of the mammary gland and gastrointestinal tract. It is also the initial product for the synthesis of 5-fluor-2''desoxyuridine and N-2''-tetrahydrofuryl-5-fluorouracil which are also employed in medicine as antitumor agents. Besides the above, 5-fluorouracil finds application for biochemical investigations.
摘要:Coote, S. C.; Smith, L. H. S.; Procter, D. J., Science of Synthesis Knowledge Updates, (2010) 3, 419. 摘要:Egart, B.; Czekelius, C., Science of Synthesis Knowledge Updates, (2013) 4, 386. 参考文献:10.1007/s00216-006-0713-x 摘要:Koryagina NL, Savelieva EI, Khlebnikova NS, Goncharov NV, Jenkins RO, Radilov AS. Determination of fluoroacetic acid in water and biological samples by GC-FID and GC-MS in combination with solid-phase microextraction. Analytical and Bioanalytical Chemistry. 2006 Aug 29;386(5):1395–400. doi: 10.1007/s00216-006-0713-x.