专利号:WO-2021108999-A1 优先权日:2019-12-03 标 题 :Method for continuous synthesis of 4-ethoxy-1,1,1-trifluoro-3-buten-2-one 发明人:HONG HAO; ZHANG ENXUAN; LU JIANGPING; SHEN WEI; YAN HONGLEI; LIU YUNPENG 权利人:LIAONING ASYMCHEM LABORATORIES CO LTD 摘要:Disclosed is a method for the continuous synthesis of 4-ethoxy-1,1,1-trifluoro-3-buten-2-one. The continuous synthesis method comprises: continuously introducing a raw material comprising vinyl ethyl ether, triethylamine and trifluoroacetic anhydride into a continuous reactor for a reaction to obtain a product system containing 4-ethoxy-1,1,1-trifluoro-3-buten-2-one, and continuously extracting the product system to obtain 4-ethoxy-1,1,1-trifluoro-3-buten-2-one. By using the continuous process, the above-mentioned raw materials can all be conveniently and accurately introduced into the continuous reactor, and after the reaction is completed, continuous extraction is also used for a post-treatment. The whole process is rapid, simple and efficient, the efficiency of the whole synthesis process is greatly increased, product destruction loss is reduced, and hidden safety hazards during batch production are avoided. After scaling up, there is no amplification effect, and safety and a relatively high synthesis efficiency can still be maintained.
专利号:US-7129357-B2 优先权日:2003-09-15 标题:Synthesis of quinoline 5-carboxamides useful for the preparation of PDE IV inhibitors 发明人:ANDREWS DAVID R; TANG SUHAN; WU WENXUE; KALLINEY SAMI Y; SUDHAKAR ANANTHA; NIELSEN CHRISTOPHER 权利人:SCHERING CORP 摘要:In one embodiment, the present application discloses a process for making the compound of the formula:
专利号:US-8981115-B2 优先权日:2008-09-30 标 题 :Process for the synthesis of halogenated cyclic compounds 发明人:BRAUN MAX 权利人:SOLVAY 摘要:A process for the manufacture of a cyclic compound of formula (I) n n n n n n n n n n which comprises (a) adding an acid halide of formula R 1 —C (O)—X, to a vinyl ether of formula (II): CH 2 â•?CH—OR 2 , to produce an addition product, and (b) reacting the addition product with a compound of formula (III): Y-A-Z; wherein R 1 is a halogenated alkyl group; wherein X is fluorine, chlorine, or bromine; wherein R 2 is an alkyl group, an aralkyl group, or an aryl group; wherein Z and Y designate independently carbon or a heteroatom; and wherein A is a linking group between Z and Y comprising 0, 1, 2 or 3 atoms in the cycle.
专利号:WO-2021152055-A1 优先权日:2020-01-31 标 题:Process for the manufacture of haloalkyl substituted pyridine compounds 发明人:JAUNZEMS JANIS; NAUERT STEFANIE; SCHMITT ETIENNE; SCHULZ ALEXANDER; CLAASSEN UTA 权利人:SOLVAY 摘要:Process for the manufacture of haloalkyl substituted pyridine compounds The present invention relates to a process for the synthesis of haloalkyl substituted pyridine compounds, a process for manufacturing a pharmaceutically or agriculturally active compound, preferably a herbicidal compound, and a haloalkyl substituted pyridine compound.
专利号:WO-2016071243-A1 优先权日:2014-11-05 标 题:Process for preparing halogenated alkenone ethers and their use in the synthesis of anthranilamide pesticides 发明人:BENSON STEFAN; ZIERKE THOMAS; GOETZ ROLAND; WALK BERNHARD; DOMRES MONIKA 权利人:BASF SE 摘要:The present invention relates to a process for preparing a compound of formula (III) starting from the vinyl ether (IlIa) and the compound (IIIb) with a reagent (lllc) selected from the group of sulfonylhalides or sulfonylanhydrides, e.g. methanesulfonyl chloride or p-toluenesulfonyl chloride, in the presence of a base. The present invention relates also to processes comprising further preceding and/or subsequent reaction steps, leading to anthranilamide pesticides or to precursors for them.
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.
参考文献:10.1007/s11696-023-03056-z 摘要:Rajmane A, Kumbhar A. Cyanomethyl pyridinium and isoquinolinium salts: a versatile chemical reagent for the synthesis of annulated heterocycles. Chem. Pap. 2023 Oct 01;78(1):35–69. doi: 10.1007/s11696-023-03056-z. 参考文献:10.1007/s11144-024-02578-1 摘要:Vdovenko SI, Gerus II, Pagacz-Kostrzewa M, Wierzejewska M. Comparison of kinetic and thermodynamic parameters of reaction of individual conformers of α-substituted β-ethoxyvinyl trifluoromethyl ketones with secondary amines. Reac Kinet Mech Cat. 2024 Feb 24;137(2):719–36. doi: 10.1007/s11144-024-02578-1. 参考文献:10.1007/s11237-026-09867-x 摘要:Vdovenko SI, Gerus II, Fedorenko EA. UV-Induced Conformational Transformations of α-Substituted β-Ethoxyvinyl Trifluoromethyl Ketones in an Argon Matrix. Theor Exp Chem. 2025 Jul;61(3):217–23. doi: 10.1007/s11237-026-09867-x.