CAS: 685-88-1; Diethyl Fluoromalonate

相似化合物

473-87-0 680-65-9 16519-02-1

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Sodium Diethylmalonate置于二氟代氙,二甲基硫,三氟化硼乙醚体系中,用 二氯甲烷 作为反应溶剂,以42%的收率获得产物2-氟丙二酸二乙酯
参考文献:在硫(II)衍生物存在下用二氟化氙氟化碳
标题:在硫(II)衍生物存在下用二氟化氙氟化碳
摘要:从二氟化氙与硫ii衍生物如二甲基硫的反应中获得能够适度氟化碳的亲电氟化试剂.
DOI:10.1016/s0022-1139(00)81611-5

专利信息

专利号:WO-2023000636-A1
优先权日:2021-07-20
标题:Method for synthesis of (3-fluorooxetan-3-yl)methyl 4-methylbenzenesulfonate
发明人：LIU YANG; WEI YUANBO; WANG QIUFENG; Xue Duoqing; WU YONG
权利人:ACCELA CHEMBIO CO LTD
摘要:A method for synthesis of (3-fluorooxetan-3-yl)methyl 4-methylbenzenesulfonate. A target product is prepared by using diethyl 2-fluoromalonate as a raw material and by means of a methylolation reaction, a hydroxyl protection reaction, a reduction reaction, an esterification reaction, a deprotection reaction, and a ring closure reaction in six steps. The steps are simple, the operation is easy, the raw material utilization rate and the product yield are high, intermediates are easy to separate, and the method is suitable for industrial scale-up production in terms of process safety, cost, raw material utilization rate, product purity, and the like. The results of embodiments show that the total yield of the reactions in the six steps of the method is 40-60%, and the HPLC purity of the target product (3-fluorooxetan-3-yl)methyl 4-methylbenzenesulfonate is greater than 97%.

专利号:US-6051704-A
优先权日:1996-07-22
标题:Synthesis of macrocyclic tetraamido-N ligands
发明人：GORDON-WYLIE SCOTT W; COLLINS TERRENCE J
权利人:UNIV CARNEGIE MELLON
摘要:New synthetic methods for the preparation of macrocyclic amido-N donor ligands are provided. The primary method of the present invention involves in general only two synthetic steps. In the first step, an α or β amino carboxylic acid is allowed to react with an optimal (approximately stoichiometric) amount of an activated malonate or oxalate derivative with mild heating. Upon completion of the double coupling reaction, hydrolysis of the reaction mixture yields a diamide containing intermediate (a macro linker). In the second step, stoichiometric amounts of a diamine, preferably an orthophenylene diamine, are added to the macro linker intermediate in the presence of a coupling agent and heat. This second double coupling reaction, is allowed to proceed for a period of time sufficient to produce a macrocyclic tetraamido compound. The substituent groups on the α or β amino carboxylic acid, the malonate, and the aryl diamine may all be selectively varied so that the resulting tetraamido macrocycle can be tailored to specific desired end uses. The macrocyclic tetraamide ligand may then be complexed with a metal, such as a transition metal, and preferably the middle and later transition metals, to form a robust chelate complex suitable for catalyzing oxidation reactions.

专利号:US-9278919-B1
优先权日:2015-03-13
标题:Synthesis of N-(3-(5-fluoro-2-(4-(2-methoxyethoxy)phenylamino)pyrimidin-4-ylamino)phenyl)acrylamide
发明人：XU YONG
权利人:XU YONG
摘要:A method for preparing BTK inhibitor CC-292 of formula 1, comprising: (1) contacting a compound of formula 2 with a compound of formula 3 to obtain a compound of formula 4; (2) contacting the compound of formula 4 with a compound of formula 5 to obtain a compound of formula 6; (3) contacting the compound of formula 6 with trifluoromethanesulfonic anhydride to obtain a compound of formula 7; and (4) contacting the compound of formula 7 with a compound of formula 8 to obtain the compound of formula 1,

专利号:US-4215044-A
优先权日:1979-04-23
标题:Synthesis of α-fluorocarbonyl compounds
发明人：MIDDLETON WILLIAM J
权利人:DU PONT
摘要:Process for preparing an organic compound of the formula R 2 R 2 CFC(O)R 3 , which process comprises contacting and reacting in a reaction mixture which includes an inert solvent, at a temperature of -40° C. to -100° C., ROF and ##STR1## R is polyfluoroperhaloalkyl of 1-6 carbon atoms or FOCF 2 ; R 1 is hydrocarbyl of 1-6 carbon atoms; n each R 2 is selected from H, alkyl of 1-17 carbon atoms, cycloalkyl of 3-6 carbon atoms, aryl, heteroaryl and such alkyl, cycloalkyl, aryl and heteroaryl substituted by halogen or alkoxy of 1-6 carbon atoms; n R 3 is selected from H, alkyl and haloalkyl of 1-16 carbon atoms, cycloalkyl of 3-10 carbon atoms, aryl and haloaryl, OSi(R 1 ) 3 , OH, NH 2 , alkoxy of 1-6 carbon atoms, aryloxy, NHR 1 and NR 1 2 wherein R 1 is alkyl of 1-6 carbon atoms, N-arylamino and nitrogen or sulfur heterocyclic of 4-5 carbon atoms; n R 3 and one R 2 taken together is a diradical which with the Câ•?C group is carbocyclic, heterocyclic or haloheterocyclic, and recovering from the reaction mixture the compound of the formula R 2 R 2 CFC()R 3 .

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:CA-2952530-A1
优先权日:2014-06-18
标题:Synthesis of halogenated malonic acid diesters and use thereof in the synthesis of 2-halogen-acrylic acid esters