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1. 发明授权

US09156771B2 Process for the preparation of enolate salts of 4-fluoro-2-hydroxymethylene-3 oxo-butyrates 有权
标题翻译：制备4-氟-2-羟基亚甲基-3-氧代 - 丁酸酯的烯醇盐的方法
公开(公告)号：US09156771B2
公开(公告)日：2015-10-13
申请号：US13809739
申请日：2011-07-11
申请人： Martina Eichenberger , Paul Hanselmann , Florencio Zaragoza Dörwald
发明人： Martina Eichenberger , Paul Hanselmann , Florencio Zaragoza Dörwald
IPC分类号： C07C51/58 , C07C51/62 , C07C67/14 , C07C67/31 , C07C67/343 , C07C69/14 , C07C69/738
CPC分类号： C07C67/31 , C07C51/58 , C07C51/62 , C07C67/14 , C07C67/343 , C07C69/14 , C07C69/738 , C07C53/48 , C07C59/21
摘要： Enolate salts of 4-fluoro-2-hydroxymethylene-3-oxobutyrates of formula wherein R1 is C1-10 alkyl, R2 and R3 are independently hydrogen or fluorine, M is an alkali or alkaline earth metal, and n is 1 or 2, are prepared from enolate salts of the corresponding 4-fluoro-3-oxobutyrates and carbon monoxide. The enolate salts of formula I can be alkylated or acylated to obtain the corresponding enol ethers and esters. The 4-fluoro-3-oxobutyrate starting material can be prepared from 1,1-difluoroethyl methyl ethers by SbF5-catalyzed fluoromethane elimination followed by halogen exchange with lithium chloride, reacting the thus obtained fluoroacetyl chloride with ketene and quenching with the appropriate alcohol R1—OH.
摘要翻译： 4-氟-2-羟基亚甲基-3-氧代丁酸烯醇盐，其中R 1是C 1-10烷基，R 2和R 3独立地是氢或氟，M是碱金属或碱土金属，n是1或2是由相应的4-氟-3-氧代丁酸乙酯和一氧化碳的烯醇盐制备。式I的烯醇盐可以被烷基化或酰化以得到相应的烯醇醚和酯。 4-氟-3-氧代丁酸酯原料可以由1,1-二氟乙基甲基醚通过SbF 5催化的氟甲烷消除制备，随后与氯化锂进行卤素交换，使得到的氟乙酰氯与乙烯酮反应，并用适当的醇R 1 -哦。

2. 发明申请

US20120035395A1 PROCESS FOR PRODUCING PHTHALIC ACID COMPOUND INCLUDING CHLORINATED AROMATIC RING 审中-公开
标题翻译：用于生产包含氯化芳族环的酸性化合物的方法
公开(公告)号：US20120035395A1
公开(公告)日：2012-02-09
申请号：US13262895
申请日：2010-04-23
申请人： Hiroshi Souda , Koji Hagiya
发明人： Hiroshi Souda , Koji Hagiya
IPC分类号： C07C51/62
CPC分类号： C07C51/62 , C07C63/68
摘要： Provided is a process for producing a phthalic acid compound whose aromatic ring has been chlorinated, the process reacting a phthalic acid compound and chlorine in a mixture of chlorosulfonic acid and thionyl chloride in the presence of an iodine compound.
摘要翻译：本发明提供一种芳族环已被氯化的邻苯二甲酸化合物的制造方法，该方法是在碘化合物的存在下，将氯苯磺酸与亚硫酰氯的混合物中的邻苯二甲酸化合物与氯反应。

3. 发明申请

US20110183956A1 PROCESS FOR THE SYNTHESIS OF EZETIMIBE AND INTERMEDIATES USEFUL THEREFOR 审中-公开
标题翻译：合成EZETIMIBE及其有用的中间体的方法
公开(公告)号：US20110183956A1
公开(公告)日：2011-07-28
申请号：US13055872
申请日：2009-07-29
申请人： Janez Mravljak , Matej Sova , Andreja Kovac , Stanislav Gobec , Zdenko Casar
发明人： Janez Mravljak , Matej Sova , Andreja Kovac , Stanislav Gobec , Zdenko Casar
IPC分类号： A61K31/397 , C07C51/62 , C07D263/26 , C07D205/08 , A61P3/06
CPC分类号： C07D263/26 , C07B2200/07 , C07C51/09 , C07C57/60 , C07C67/343 , C07C69/65 , C07D205/08
摘要： The present invention discloses novel and useful intermediates for the synthesis of ezetimibe (EZT), which intermediates share a characteristic Z-isomeric structure. Based on Z-5-(4-fluorophenyl)-pent-4-enoic acid, and proceeding the synthesis through further Z-intermediates, a total synthesis is presented to obtained final ezetimibe in high yields.
摘要翻译：本发明公开了用于合成依泽替米贝（EZT）的新型有用的中间体，其中间体具有特征的Z-异构体结构。基于Z-5-（4-氟苯基） - 戊-4-烯酸，并通过进一步的Z-中间体进行合成，总共合成以高产率得到最终的依泽替米贝。

4. 发明授权

US06919479B2 Process for the preparation of perfluoropolyethers acyl-fluoride ended by reduction of the corresponding peroxidic perfluoropolyethers 失效
标题翻译：制备全氟聚醚酰氟的方法是通过还原相应的过氧化全氟聚醚来终止
公开(公告)号：US06919479B2
公开(公告)日：2005-07-19
申请号：US10631862
申请日：2003-08-01
申请人： Antonella Di Meo , Rosaldo Picozzi , Claudio Tonelli
发明人： Antonella Di Meo , Rosaldo Picozzi , Claudio Tonelli
IPC分类号： C07C51/62 , C07B61/00 , C07C59/135 , C08G65/00 , C08G65/22 , C08G65/322 , C07C51/09
CPC分类号： C08G65/226 , C08G65/007 , C08G65/322
摘要： A process for the preparation of perfluoropolyethers of formula: T-CFX′—O—Rf—CFX—COF (I) wherein: T=COF, F, C1-C3 perfluoroalkyl; X, X′=—F, —CF3; Rf=—(C2F4O)m(CF2CF(CF3)O)n(CF2O)p(CF(CF3)O)q—, the sum n+m+p+q ranges from 2 to 200, by reduction with hydrogen of the corresponding peroxidic perfluoropolyethers, in the presence of a catalyst formed by metals of the VIII group supported on metal fluorides, at a temperture from 20° C. to 140° C., and at a pressure between 1 and 50 atm.
摘要翻译：一种制备式的全氟聚醚的方法：<？in-line-formula description =“In-line formula”end =“lead”？> T-CFX'-ORF-CFX-COF （I）<？in-line-formula description =“In-line Formulas”end =“tail”？>其中：T = COF，F，C 1 -C 3，全氟烷基 X，X'= -F，-CF 3 3; （CF 2）2 - （C 2 H 4）（CF 2） CF（CF 3）O）n（CF 2 O）p（CF 3 CF 3）通过在相应的过氧化全氟聚醚的氢还原的情况下，在由下述催化剂形成的催化剂的存在下，n + m + p + q的和n + m + p + q在2至200的范围内， VIII族的金属在金属氟化物上负载，温度为20℃至140℃，压力为1至50atm。

5. 发明授权

US6066764A Production of 3-chloro-4-fluoro-benzoyl chloride by Lewis-acid catalyzed chlorination of the aromatic ring 有权
标题翻译：通过路易斯酸催化氯化芳环制备3-氯-4-氟 - 苯甲酰氯
公开(公告)号：US6066764A
公开(公告)日：2000-05-23
申请号：US151645
申请日：1998-09-10
申请人： Dino Bonini , Damiano Torrente , Filippo Maria Carlini
发明人： Dino Bonini , Damiano Torrente , Filippo Maria Carlini
IPC分类号： B01J27/10 , C07B61/00 , C07C51/62 , C07C51/64 , C07C63/70 , C07C51/58
CPC分类号： C07C63/70 , C07C51/62 , Y02P20/582
摘要： The present invention relates to halogenated aromatic derivatives, in particular 3-chloro-4-fluoro-benzoyl chloride having the following formula: ##STR1## The aforesaid derivative is advantageously used as base product for the preparation of fluorinated compounds employed in their turn as active principles in the pharmaceutical and agricultural fields as well as in dye industry.The present invention also relates to a process for the preparation of 3-chloro-4-fluoro-benzoyl chloride that allows to obtain the end compound with high selectivity, high yields and one only step starting from a known and commercially available product
摘要翻译：本发明涉及卤代芳族衍生物，特别是具有下式的3-氯-4-氟 - 苯甲酰氯：上述衍生物有利地用作制备作为本发明的活性成分的氟化合物的基础产物制药和农业领域以及染料行业。本发明还涉及一种制备3-氯-4-氟 - 苯甲酰氯的方法，其允许以高选择性，高产率获得末端化合物，并且从已知和市售产品开始仅一步

6. 发明授权

US5969200A Process for the manufacture of acetonylbenzamides 失效
标题翻译：丙酮基苯甲酰胺的制备方法
公开(公告)号：US5969200A
公开(公告)日：1999-10-19
申请号：US176821
申请日：1998-10-22
申请人： Enrique Luis Michelotti , Heather Lynnette Rayle , Randall Wayne Stephens , William Joseph Zabrodski
发明人： Enrique Luis Michelotti , Heather Lynnette Rayle , Randall Wayne Stephens , William Joseph Zabrodski
IPC分类号： C07C51/62 , C07C205/57 , C07C205/58 , C07C205/59 , C07C205/61 , C07C17/00
CPC分类号： C07C205/61 , C07C201/12 , C07C205/57 , C07C205/58 , C07C205/59 , C07C221/00 , C07C227/10 , C07C51/62
摘要： Novel routes for the preparation of acetonylbenzamides are provided by the reaction of an amine and acyl chloride. Novel routes to various intermediates used in the manufacture of acetonylbenzamides are also disclosed.
摘要翻译：用于制备丙酮基苯甲酰胺的新途径是通过胺和酰氯的反应来提供的。还公开了用于制备丙酮基苯甲酰胺的各种中间体的新途径。

7. 发明授权

US5945565A Process for the manufacture of acetonylbenzamides 失效
公开(公告)号：US5945565A
公开(公告)日：1999-08-31
申请号：US177149
申请日：1998-10-22
申请人： Enrique Luis Michelotti , Heather Lynnette Rayle , Randall Wayne Stephens , William Joseph Zabrodski
发明人： Enrique Luis Michelotti , Heather Lynnette Rayle , Randall Wayne Stephens , William Joseph Zabrodski
IPC分类号： B01J31/02 , C07B61/00 , C07C51/62 , C07C205/57 , C07C205/58 , C07C205/59 , C07C231/02 , C07C231/04 , C07C233/76 , C07C235/44 , C07C237/30 , C07C249/08 , C07C251/48 , C07C51/58
CPC分类号： C07C51/62 , C07C201/12 , C07C221/00 , C07C227/10 , C07C231/02 , C07C249/08
摘要： Novel routes for the preparation of acetonylbenzamides are provided by the reaction of an amine and acyl chloride. Novel routes to various intermediates used in the manufacture of acetonylbenzamides are also disclosed.

8. 发明授权

US5055601A Fluoroepoxides and a process for production thereof 失效
标题翻译：氟代氧化物及其生产方法
公开(公告)号：US5055601A
公开(公告)日：1991-10-08
申请号：US442373
申请日：1989-11-28
申请人： Masanori Ikeda , Morikazu Miura , Atsushi Aoshima
发明人： Masanori Ikeda , Morikazu Miura , Atsushi Aoshima
IPC分类号： C07C51/41 , C07C51/58 , C07C51/62 , C07D303/08 , C07D303/48
CPC分类号： C07D301/14 , C07C51/41 , C07C51/58 , C07C51/62 , C07D303/48
摘要： A process for epoxidation of a fluoro-olefin is disclosed. The process comprises epoxidizing a fluoro-olefin represented by the general formula (I): ##STR1## wherein X.sup.1, X.sup.2 and X.sup.3 each represents a substituent selected from (a)--F, (b) a perfluoroalkyl group having 2 to 20 carbon atoms and (c) --CF.sub.2 Y.sup.1, Y.sup.1 may be the same or different and represents a substituent selected from (d) a halogen atom selected from F, Cl, Br and I, (e) --OZ.sup.1 and (f) --Z.sup.1, wherein Z.sup.1 may be the same or different and represents a substituted or unsubstituted hydrocarbon group having not more than 20 carbon atoms, and X.sup.1, X.sup.2, X.sup.3 and Y.sup.1 may be combined with one another to form a cyclic compound, provided that all of X.sup.1, X.sup.2, X.sup.3 and Y.sup.1 do not represent --F; using a hypochlorite dissolved or suspended in an aqueous phase as an oxidizing agent in the presence or absence of an inorganic base. The reaction is performed in a two phase system (aqueous and organic phases) in the presence of at least one phase transfer catalyst selected from (i) quaternary ammonium salts, (ii) quaternary phosphonium salts, (iii) quaternary arsonium salts, (iv) sulfonium salts and (v) lipophilic complexing agents for cations contained in the hypochlorite.

9. 发明授权

US4965379A Fluoroepoxides and a process for production thereof 失效
标题翻译：氟环氧化物及其制备方法
公开(公告)号：US4965379A
公开(公告)日：1990-10-23
申请号：US69745
申请日：1987-07-06
申请人： Masanori Ikeda , Morikazu Miura , Atsushi Aoshima
发明人： Masanori Ikeda , Morikazu Miura , Atsushi Aoshima
IPC分类号： C07C51/41 , C07C51/58 , C07C51/62 , C07D303/08 , C07D303/48
CPC分类号： C07D301/14 , C07C51/41 , C07C51/58 , C07C51/62 , C07D303/48
摘要： A process for epoxidation of a fluoro-olefin is disclosed. The process comprises epoxidizing a fluoro-olefin represented by the general formula (I): ##STR1## wherein X.sup.1, X.sup.2 and X.sup.3 each represents a substituent selected from (a) --F, (b) a perfluoroalkyl group having 2 to 20 carbon atoms and (c) --CF.sub.2 Y.sup.1, Y.sup.1 may be the same or different and represents a substituent selected from (d) a halogen atom selected from F, Cl, Br and I, (e) --OZ.sup.1 and (f) --Z.sup.1, wherein Z.sup.1 may be the same or different and represents a substituted or unsubstituted hydrocarbon group having not more than 20 carbon atoms, and X.sup.1, X.sup.2, X.sup.3 and Y.sup.1 may be combined with one another to form a cyclic compound, provided that all of X.sup.1, X.sup.2, X.sup.3 and Y.sup.1 do not represent --F; using a hypochlorite dissolved or suspended in an aqueous phase as an oxidizing agent in the presence or absence of an inorganic base. The reaction is performed in a two phase system (aqueous and organic phases) in the presence of at least one phase transfer catalyst selected from (i) quaternary ammonium salts, (ii) quaternary phosphonium salts, (iii) quaternary arsonium salts, (iv) sulfonium salts and (v) lipophilic complexing agents for cations contained in the hypochlorite.
摘要翻译：公开了氟代烯烃的环氧化方法。该方法包括环氧化由通式（I）表示的氟代烯烃：其中X 1，X 2和X 3各自表示选自（a）-F，（b）具有2〜 20个碳原子和（c）-CF 2 Y 1，Y 1可以相同或不同，表示选自（d）选自F，Cl，Br和I的卤素原子，（e）-OZ1和（f）-Z1 其中Z1可以相同或不同，表示具有不超过20个碳原子的取代或未取代的烃基，X1，X2，X3和Y1可以相互结合形成环状化合物，条件是全部X1 ，X2，X3和Y1不表示-F; 在存在或不存在无机碱的情况下，使用溶解或悬浮在水相中的次氯酸盐作为氧化剂。在至少一种相转移催化剂的存在下，在两相体系（水相和有机相）中进行反应，所述相转移催化剂选自（i）季铵盐，（ii）季鏻盐，（iii）季ium盐，（iv ）锍盐和（v）用于次氯酸盐中所含阳离子的亲脂性络合剂。

10. 发明授权

US4322374A 2,4,4,4-Tetrahalobutanoic acid halide 失效
标题翻译： 2,4,4,4-四卤丁酸卤化物
公开(公告)号：US4322374A
公开(公告)日：1982-03-30
申请号：US181015
申请日：1980-08-25
申请人： Pierre Martin , Hans Greuter , Eginhard Steiner , Daniel Bellus
发明人： Pierre Martin , Hans Greuter , Eginhard Steiner , Daniel Bellus
IPC分类号： C07C51/60 , C07C51/62 , C07C53/50 , C07C61/15 , C07C61/40
CPC分类号： C07C45/45 , C07C45/67 , C07C51/60 , C07C51/62 , C07C53/50 , C07C61/15 , C07C61/40
摘要： The preparation and use as an intermediate for making insecticides has been disclosed for a compound of the formula: ##STR1## in which X and Y are each chlorine or bromine.
摘要翻译：已经公开了制备和用作制备杀虫剂的中间体的下式化合物：其中X和Y各自为氯或溴。

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