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1. 发明授权

US10112948B2 Benzamide or benzamine compounds useful as anticancer agents for the treatment of human cancers 有权
公开(公告)号：US10112948B2
公开(公告)日：2018-10-30
申请号：US15194825
申请日：2016-06-28
申请人： THE BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM
发明人： Jef DeBrabander , Luis Parada
IPC分类号： C07D487/04 , C07D213/16 , C07D207/09 , C07C323/22 , C07D295/13 , C07D401/12 , C07C205/58 , C07D213/70 , C07C255/57 , C07D307/14 , C07D209/48 , C07C235/50 , C07C205/61 , C07D211/14 , C07C271/20 , C07C323/62
摘要： The described invention provides small molecule anti-cancer compounds for treating tumors that respond to cholesterol biosynthesis inhibition. The compounds selectively inhibit the cholesterol biosynthetic pathway in tumor-derived cancer cells, but do not affect normally dividing cells.

2. 发明授权

US09394240B2 Method for producing amide derivative 有权
标题翻译：酰胺衍生物的制备方法
公开(公告)号：US09394240B2
公开(公告)日：2016-07-19
申请号：US14306885
申请日：2014-06-17
申请人： Mitsui Chemicals Agro, Inc.
发明人： Youji Aoki , Yumi Kobayashi , Hidenori Daido , Hiroyuki Katsuta , Hidetaka Tsukada , Atsushi Hirabayashi , Yusuke Takahashi , Michikazu Nomura , Atsuko Kawahara
IPC分类号： C07C237/28 , C07C235/68 , A01N37/46 , A01N43/40 , C07C205/58 , C07C231/02 , C07C233/81 , C07C255/57 , C07D213/82 , C07C255/58
CPC分类号： C07C233/76 , A01N37/46 , A01N43/40 , C07C205/58 , C07C231/02 , C07C233/81 , C07C235/68 , C07C255/57 , C07C255/58 , C07D213/82 , C07C237/42
摘要： An amide derivative represented by Formula (3), which exhibits excellent efficacy in pest control effect, is produced by allowing a compound represented by the following Formula (1) and a compound represented by Formula (2) to react with each other. In Formula (1) to Formula (3), Y1 and Y2 each represent a halogen atom or a haloalkyl group; Rf represents a C3-C4 perfluoroalkyl group; and R1 and R2 each represent a hydrogen atom or an alkyl group; LG represents a leaving group; T represents a hydrogen atom or a fluorine atom; X1, X3, X4, and X5 each represent a hydrogen atom, a halogen atom, or the like; and A represents a nitrogen atom, a methine group, or the like.
摘要翻译：通过使由下式（1）表示的化合物和由式（2）表示的化合物彼此反应来制备在害虫防治效果上显示出优异效果的由式（3）表示的酰胺衍生物。在式（1）至式（3）中，Y 1和Y 2各自表示卤原子或卤代烷基; Rf表示C3-C4全氟烷基; 并且R 1和R 2各自表示氢原子或烷基; LG代表离职团体; T表示氢原子或氟原子; X1，X3，X4和X5各自表示氢原子，卤素原子等; A表示氮原子，次甲基等。

3. 发明授权

US08853440B2 Method for producing amide derivative 有权
标题翻译：酰胺衍生物的制备方法
公开(公告)号：US08853440B2
公开(公告)日：2014-10-07
申请号：US13058349
申请日：2009-08-13
申请人： Youji Aoki , Yumi Kobayashi , Hidenori Daido , Hiroyuki Katsuta , Hidetaka Tsukada , Atsushi Hirabayashi , Yusuke Takahashi , Michikazu Nomura , Atsuko Kawahara
发明人： Youji Aoki , Yumi Kobayashi , Hidenori Daido , Hiroyuki Katsuta , Hidetaka Tsukada , Atsushi Hirabayashi , Yusuke Takahashi , Michikazu Nomura , Atsuko Kawahara
IPC分类号： C07C231/02 , C07D213/82 , C07C233/81 , A01N37/46 , C07C255/57 , C07C205/58 , A01N43/40
CPC分类号： C07C233/76 , A01N37/46 , A01N43/40 , C07C205/58 , C07C231/02 , C07C233/81 , C07C235/68 , C07C255/57 , C07C255/58 , C07D213/82 , C07C237/42
摘要： An amide derivative represented by Formula (3), which exhibits excellent efficacy in pest control effect, is produced by allowing a compound represented by the following Formula (1) and a compound represented by Formula (2) to react with each other. In Formula (1) to Formula (3), Y1 and Y2 each represent a halogen atom or a haloalkyl group; Rf represents a C3-C4 perfluoroalkyl group; and R1 and R2 each represent a hydrogen atom or an alkyl group; LG represents a leaving group; T represents a hydrogen atom or a fluorine atom; X1, X3, X4, and X5 each represent a hydrogen atom, a halogen atom, or the like; and A represents a nitrogen atom, a methine group, or the like.
摘要翻译：通过使由下式（1）表示的化合物和由式（2）表示的化合物彼此反应来制备在害虫防治效果上显示出优异效果的由式（3）表示的酰胺衍生物。在式（1）至式（3）中，Y 1和Y 2各自表示卤原子或卤代烷基; Rf表示C3-C4全氟烷基; 并且R 1和R 2各自表示氢原子或烷基; LG代表离职团体; T表示氢原子或氟原子; X1，X3，X4和X5各自表示氢原子，卤素原子等; A表示氮原子，次甲基等。

4. 发明申请

US20100145065A1 PROCESS FOR PREPARING BENZIMIDAZOLE COMPOUNDS 有权
标题翻译：制备苯并咪唑化合物的方法
公开(公告)号：US20100145065A1
公开(公告)日：2010-06-10
申请号：US11993745
申请日：2006-06-21
申请人： John Demattei , Sagar Shakya , Anthony D. Piscopio , Bruno P. Hache , Matthew Charles Evans , James Gair Ford , Simon Mark Pointon , Koen Peeters , Timothy John Lilley , John Leonard
发明人： John Demattei , Sagar Shakya , Anthony D. Piscopio , Bruno P. Hache , Matthew Charles Evans , James Gair Ford , Simon Mark Pointon , Koen Peeters , Timothy John Lilley , John Leonard
IPC分类号： C07D235/04 , C07C229/60 , C07C205/58
CPC分类号： C07D235/06 , C07C201/08 , C07C205/58 , C07C227/04 , C07C227/08 , C07C227/18 , C07C229/60
摘要： Provided are methods for the synthesis of heterocyclic compounds such as benzimidazole carboxylic acid core structures having Formula Ia-1 and their synthetic intermediates: wherein Z, X1, X2, X5, R2 and R10 are as defined herein. Compounds of Formula Ia-1 and their synthetic intermediates can be used to prepare heterocyclic derivatives such as benzimidazole derivatives.
摘要翻译：提供了用于合成杂环化合物的方法，例如具有式Ia-1的苯并咪唑羧酸核心结构及其合成中间体：其中Z，X1，X2，X5，R2和R10如本文所定义。式Ia-1及其合成中间体的化合物可用于制备杂环衍生物如苯并咪唑衍生物。

5. 发明授权

US5637765A Process for the preparation of fluorinated benzoic acids 失效
标题翻译：氟代苯甲酸的制备方法
公开(公告)号：US5637765A
公开(公告)日：1997-06-10
申请号：US462235
申请日：1995-06-05
申请人： Xiu C. Wang , Panos Kalaritis , Michelle L. Chang
发明人： Xiu C. Wang , Panos Kalaritis , Michelle L. Chang
IPC分类号： C07C51/363 , C07C205/12 , C07C205/45 , C07C205/56 , C07C205/58 , C07C255/35 , C07C205/00
CPC分类号： C07C255/35 , C07C205/12 , C07C205/45 , C07C205/56 , C07C205/58 , C07C51/363
摘要： A process for the preparation of 2-chloro-4,5-difluorobenzoic acid and 2,4,5-trifluorobenzoic acid as well as synthetic intermediates useful in and prepared according thereto, comprising reacting a nitrobenzene having the formula ##STR1## wherein X is chloro or fluoro, with an appropriate carbanion to form a compound having the formula ##STR2## wherein one of Y and Z is chloro and the other is nitro, and R is a radical selected from the group consisting of --CCl.sub.3, --CH.sub.2 NO.sub.2, --CH(NO.sub.2)R.sup.1, --CH(CO.sub.2 R.sup.1).sub.2, --CH(C(O)R.sup.2).sub.2, --CH(CN)CO.sub.2 R.sup.1, --CH(CO.sub.2 R.sup.1)COR.sup.2 and --COR.sup.2 where R.sup.1 is alkyl or arylalkyl and R.sup.2 is alkyl, aryl or arylalkyl and, where appearing more than once in such a radical, R.sup.1 and R.sup.2 may be the same or different at each occurrence.
摘要翻译：一种制备2-氯-4,5-二氟苯甲酸和2,4,5-三氟苯甲酸的方法，以及可用于和制备的合成中间体，包括使具有下式的硝基苯：其中X为氯或氟，与适当的碳负离子形成具有下式的化合物：硝基，R是选自-CCl 3，-CH 2 NO 2，-CH（NO 2）R 1，-CH（CO 2 R 1） 2，-CH（C（O）R 2）2，-CH（CN）CO 2 R 1，-CH（CO 2 R 1）COR 2和-COR 2，其中R 1是烷基或芳基烷基，R 2是烷基，芳基或芳烷基，并且其中出现多于一次在这样的基团中，R 1和R 2可以在每次出现时相同或不同。

6. 发明授权

US5591890A Process for producing ortho-nitro aromatic acids by oxidation of ortho-nitroalkylaromatic compounds 失效
标题翻译：通过邻硝基烷基芳族化合物的氧化生产邻硝基芳香酸的方法
公开(公告)号：US5591890A
公开(公告)日：1997-01-07
申请号：US552420
申请日：1995-11-03
申请人： Stephen E. Jacobson
发明人： Stephen E. Jacobson
IPC分类号： C07C205/57 , C07C205/58 , C07C51/16
CPC分类号： C07C201/12 , C07C315/04
摘要： A process for preparing o-nitroaromatic acids by direct oxidation of the corresponding o-nitroalkylaromatic compounds, utilizing salts of certain catalytic metals in the presence of an oxygen-containing gas and an aliphatic aldehyde or ketone at elevated temperature and pressure, is provided. The process allows catalyst recovery and reuse.
摘要翻译：提供了一种通过在升高的温度和压力下在含氧气体和脂族醛或酮的存在下利用某些催化金属的盐直接氧化相应的邻硝基烷基芳族化合物来制备邻硝基芳族酸的方法。该方法允许催化剂回收和再利用。

7. 发明授权

US5481032A Process for the preparation of halogenated benzoic acids 失效
标题翻译：卤代苯甲酸的制备方法
公开(公告)号：US5481032A
公开(公告)日：1996-01-02
申请号：US159087
申请日：1993-11-29
申请人： Ralf Pfirmann
发明人： Ralf Pfirmann
IPC分类号： C07C37/60 , C07C51/285 , C07C63/70 , C07C63/72 , C07C65/03 , C07C65/21 , C07C65/30 , C07C67/29 , C07C69/035 , C07C201/12 , C07C205/58 , C07C227/02 , C07C229/54 , C07C231/12 , C07C233/65 , C07C235/46 , C07C237/30 , C07C253/30 , C07C255/57 , C07C315/04 , C07C317/44 , C07C229/52
CPC分类号： C07C51/285 , C07C37/50 , C07C41/16 , Y02P20/582
摘要： A process for the preparation of halogenated benzoic acids of formula (1): ##STR1## in which R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are hydrogen, fluorine, chlorine or bromine atoms or C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, nitro, cyano, trifluoromethyl, aidehyde, C.sub.1 -C.sub.4 -alkoxycarbonyl, -SO.sub.2 -C.sub.1 -C.sub.4 -alkyl, -SO.sub.2 -phenyl, -CONH.sub.2, -CON(C.sub.1 -C.sub.4 -alkyl).sub.2, hydroxy, carboxy, -NH.sub.2 or -N(C.sub.1 -C.sub.4 - alkyl).sub.2 groups, at least one of the substituents R.sub.1 -R.sub.5 being one of said halogen atoms, which comprises reacting 1 mol of a benzophenone, asymmetrically substituted on the benzene rings A and B, of general formula (2): ##STR2## in which R.sup.1 -R.sup.10 are as defined above for R.sub.1 -R.sub.5, with about 1 to about 10 mol of an oxidizing agent selected from the group comprising hydrogen peroxide, urea/hydrogen peroxide addition product, an alkali metal peroxide, ammonium, alkali metal or alkaline earth metal peroxodisulfates, pertungstates, perborates or percarbonates, ozone, alkyl- or aryl-percarboxylic acids, alkyl- or aryl-persulfonic acids or persulfuric acid, at temperatures from about -20.degree. to about +100.degree. C.
摘要翻译：制备式（1）的卤代苯甲酸的方法：其中R1，R2，R3，R4和R5是氢，氟，氯或溴原子或C1-C6-烷基，C1- C 1 -C 4烷氧基，硝基，氰基，三氟甲基，脱氢，C 1 -C 4烷氧基羰基，-SO 2 -C 1 -C 4烷基，-SO 2 - 苯基，-CONH 2，-CON（C 1 -C 4烷基）2，羟基，羧基， -NH 2或-N（C 1 -C 4 - 烷基）2基团，至少一个取代基R 1 -R 5是所述卤素原子之一，其包括使1摩尔苯苯酮在苯环A和B上不对称取代，的通式（2）：其中R 1 -R 10如上文对R 1 -R 5所定义，其中约1至约10mol氧化剂选自过氧化氢，尿素/过氧化氢加成产物，碱金属过氧化物，铵，碱金属或碱土金属过氧二硫酸盐，过钨酸盐，过硼酸盐或过碳酸盐，臭氧，烷基或芳基过羧酸，烷基或芳基 - 磺酸或说服在约-20℃至约+ 100℃的温度下，

8. 发明授权

US5198575A Preparation of nitrobenzoic and anthranilic acids 失效
标题翻译：硝基苯甲酸和壬二酸的制备
公开(公告)号：US5198575A
公开(公告)日：1993-03-30
申请号：US912196
申请日：1992-07-13
申请人： Helmut Hagen , Jacques Dupuis
发明人： Helmut Hagen , Jacques Dupuis
IPC分类号： B01J23/22 , B01J27/053 , C07B61/00 , C07C201/12 , C07C205/57 , C07C205/58 , C07C227/04 , C07C227/06 , C07C227/12 , C07C229/56 , C07C229/60
CPC分类号： C07C201/12 , C07C227/04
摘要： Nitrobenzoic acids I ##STR1## (X.sup.1, X.sup.2 =fluorine, chlorine, bromine, hydrogen or nitro) are prepared by oxidizing the corresponding nitrotoluene II ##STR2## with nitric acid in the presence of sulfuric acid and vanadium(V) compounds, and anthranilic acids III ##STR3## (Y.sup.1, Y.sup.2 =fluorine, chlorine, bromine, hydrogen or amino) are prepared from the nitrobenzoic acids I by reduction.
摘要翻译：通过在硫酸和钒（V）化合物的存在下用硝酸氧化相应的硝基甲苯II II，制备硝基苯甲酸I（X 1，X 2 =氟，氯，溴，氢或硝基）并且通过还原由硝基苯甲酸I制备邻氨基苯甲酸III（Y1，Y2 =氟，氯，溴，氢或氨基）。

9. 发明授权

US5006158A Certain 2-(2-substituted benzoyl)-1,3-cyclohexanediones 失效
标题翻译：某些2-（2-取代苯甲酰基）-1,3-环己烷二酮
公开(公告)号：US5006158A
公开(公告)日：1991-04-09
申请号：US128128
申请日：1988-02-23
申请人： Charles G. Carter , David L. Lee , William J. Michaely , Gary W. Kraatz
发明人： Charles G. Carter , David L. Lee , William J. Michaely , Gary W. Kraatz
IPC分类号： A01N35/06 , A01N37/48 , A01N41/06 , A01N41/10 , C07C45/45 , C07C45/54 , C07C45/72 , C07C49/792 , C07C49/813 , C07C49/835 , C07C49/84 , C07C69/76 , C07C205/06 , C07C205/45 , C07C205/57 , C07C205/58 , C07C205/59 , C07C205/61 , C07C225/22 , C07C233/33 , C07C255/56 , C07C317/44 , C07C323/62 , C07D317/52
CPC分类号： C07D317/52 , A01N35/06 , A01N37/48 , A01N41/06 , A01N41/10 , C07C205/45 , C07C205/57 , C07C205/58 , C07C205/59 , C07C205/61 , C07C225/22 , C07C233/33 , C07C255/00 , C07C255/56 , C07C317/00 , C07C317/44 , C07C323/62 , C07C45/455 , C07C45/54 , C07C45/72 , C07C49/792 , C07C49/813 , C07C49/835 , C07C49/84 , C07C69/76 , C07C2101/14
摘要： Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen or C.sub.1 -C.sub.4 alkyl; R.sup.2 is hydrogen, C.sub.1 -C.sub.4 alkyl or ##STR2## wherein R.sup.a is C.sub.1 -C.sub.4 alkyl; R.sup.1 and R.sup.2 together are alkylene having 3 to 6 carbon atoms; R.sup.3 is hydrogen or C.sub.1 -C.sub.4 alkyl; R.sup.4 is hydrogen or C.sub.1 -C.sub.4 alkyl; R.sup.5 is hydrogen or C.sub.1 -C.sub.4 alkyl; R.sup.6 is hydrogen or C.sub.1 -C.sub.4 alkyl; R.sup.7 is hydrogen or 3-C.sub.1 -C.sub.4 alkoxy; and R.sup.8 is (1) hydrogen; (2) halogen; (3) C.sub.1 -C.sub.4 alkyl; (4) C.sub.1 -C.sub.4 alkoxy; (5) OCF.sub.3 ; (6) cyano; (7) nitro; (8) C.sub.1 -C.sub.4 haloalkyl; (9) R.sup.b SO.sub.n -- wherein n is the integer 0, 1 or 2; and R.sup.b is (a) C.sub.1 -C.sub.4 alkyl; (b) C.sub.1 -C.sub.4 alkyl substituted with halogen or cyano; (c) phenyl; or (d) benzyl; (10) --NR.sup.c R.sup.d wherein R.sup.c and R.sup.d independently are hydrogen or C.sub.1 -C.sub.4 alkyl; (11) R.sup.e C(O)-- wherein R.sup.e is C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy; or (12) SO.sub.2 NR.sup.c R.sup.d wherein R.sup.c and R.sup.d are as defined, their use as herbicides and herbicidal compositions containing the compounds.
摘要翻译：其中R 1是氢或C 1 -C 4烷基的式IMAMA的化合物; R 2是氢，C 1 -C 4烷基或者其中R a是C 1 -C 4烷基; R 1和R 2一起是具有3至6个碳原子的亚烷基; R3是氢或C1-C4烷基; R4是氢或C1-C4烷基; R5是氢或C1-C4烷基; R6是氢或C1-C4烷基; R7是氢或3-C1-C4烷氧基; R8为（1）氢; （2）卤素; （3）C 1 -C 4烷基; （4）C1-C4烷氧基; （5）OCF3; （6）氰基; （7）硝基; （8）C 1 -C 4卤代烷基; （9）RbSO n-，其中n是整数0,1或2; 并且R b是（a）C 1 -C 4烷基; （b）被卤素或氰基取代的C 1 -C 4烷基; （C）苯基; 或（d）苄基; （10）-NRcRd其中Rc和Rd独立地是氢或C1-C4烷基; （11）ReC（O） - 其中Re为C1-C4烷基或C1-C4烷氧基; 或（12）SO2NRcRd，其中Rc和Rd如上所定义，它们作为除草剂和含有该化合物的除草组合物的用途。

10. 发明授权

US4868347A Process for obtaining substituted fluorobenzenes 失效
标题翻译：获得取代氟苯的方法
公开(公告)号：US4868347A
公开(公告)日：1989-09-19
申请号：US130700
申请日：1987-12-09
申请人： Heinz U. Blank , Edwin Ritzer
发明人： Heinz U. Blank , Edwin Ritzer
IPC分类号： C07C69/76 , C07B63/00 , C07C17/00 , C07C17/38 , C07C25/13 , C07C45/00 , C07C45/80 , C07C49/80 , C07C51/64 , C07C63/00 , C07C63/10 , C07C63/70 , C07C67/00 , C07C67/58 , C07C201/00 , C07C201/16 , C07C205/12 , C07C205/58 , C07C233/65 , C07C253/00 , C07C253/34 , C07C255/49 , C07C255/50 , C07C255/58 , C07C311/00 , C07C313/00 , C07C315/06 , C07C317/14 , C07C317/44
CPC分类号： C07C17/38 , C07C201/12 , C07C201/16 , C07C253/34 , C07C317/00 , C07C45/80 , C07C51/64 , C07C63/70
摘要： Substituted fluorobenzenes which are produced in aprotic, polar solvents or in mixtures which contain such solvents can be obtained by extracting the substituted fluorobenzenes from the solvents or solvent mixtures with aliphatic extracting agents and then seaprating the extracting agents from the substituted fluorobenzenes.
摘要翻译：在非质子极性溶剂或含有这些溶剂的混合物中制备的取代氟苯可以通过从溶剂或溶剂混合物中提取取代的氟苯与脂肪族萃取剂，然后从取代的氟苯中渗出萃取剂来获得。

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