Method for production of aryl-substituted annelated pyrimidines
    51.
    发明申请
    Method for production of aryl-substituted annelated pyrimidines 审中-公开
    芳基取代的环状嘧啶的制备方法

    公开(公告)号:US20100087640A1

    公开(公告)日:2010-04-08

    申请号:US12521877

    申请日:2008-01-10

    IPC分类号: C07D487/04

    CPC分类号: C07D487/04

    摘要: The present invention relates to a process for preparing aryl-substituted fused pyrimidines of the general formula (I) in which L1 to L5 are H, halogen, CN, NO2, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy etc.; Y1 to Y3 are C—RY or N; RY is H or optionally substituted C1-C4-alkyl or two adjacent RY together form a ring; X is OH, Cl or Br; which comprises (i) the reaction of a 2-phenylmalonate with a compound (III) or a tautomer thereof, in the presence of a suitable base, where the alcohol, released during the reaction, of the formula R—OH is continuously removed from the reaction mixture under reduced pressure; giving a compound of the formula (I) or a salt thereof in which X is OH, and, if X in the compounds of the general formula (I) is chlorine or bromine, (ii) the reaction of the compounds of the formula (I) obtained in step (i) or the salts with a halogenating agent.

    摘要翻译: 本发明涉及制备通式(I)的芳基取代的稠合嘧啶的方法,其中L 1至L 5为H,卤素,CN,NO 2,C 1 -C 4烷基,C 1 -C 4卤代烷基,C 1 -C 4 - 烷氧基,C1-C4-卤代烷氧基等; Y1至Y3为C-RY或N; RY为H或任选取代的C 1 -C 4烷基或两个相邻的RY一起形成环; X是OH,Cl或Br; 其包括(i)2-苯基丙二酸酯与化合物(III)或其互变异构体在合适的碱的存在下反应,其中反应期间释放的醇与式R-OH的连续从 减压下的反应混合物; 得到其中X是OH的式(I)化合物或其盐,并且如果通式(I)的化合物中的X是氯或溴,则(ii)式(I)化合物 I)或与卤化剂的盐。

    Method for the production of halogen-substituted 2-(aminomethylidene)-3-oxobutyric acid esters
    53.
    发明授权
    Method for the production of halogen-substituted 2-(aminomethylidene)-3-oxobutyric acid esters 有权
    卤素取代的2-(氨基亚甲基)-3-氧代丁酸酯的制备方法

    公开(公告)号:US08586750B2

    公开(公告)日:2013-11-19

    申请号:US12990364

    申请日:2009-04-30

    CPC分类号: C07D295/145 C07D231/14

    摘要: The present invention relates to a process for preparing 2-(aminomethylidene)-4,4-dihalo-3-oxobutyric esters of the formula (I), wherein R1, R2, R3 are C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C3-C10-cycloalkyl or benzyl, and/or R2 together with R3 and the nitrogen atom to which the two radicals are attached are a heterocyclic radical, in which a corresponding 3-aminoacrylic ester is reacted with a halogen-substituted acetyl fluoride in the presence of at least one alkali or alkaline earth metal fluoride; and the further conversion of halogen-substituted 2-(aminomethylidene)-3-oxobutyric esters of the formula (I) to halomethyl-substituted pyrazol-4-ylcarboxylic acids and their esters.

    摘要翻译: 本发明涉及制备式(I)的2-(氨基亚甲基)-4,4-二卤代-3-氧代丁酸酯的方法,其中R1,R2,R3是C1-C6-烷基,C1-C6-卤代烷基 ,C 2 -C 6 - 烯基,C 3 -C 10 - 环烷基或苄基,和/或R 2与R 3和两个基团所连接的氮原子是杂环基团,其中相应的3-氨基丙烯酸酯与 卤素取代的乙酰氟在至少一种碱金属或碱土金属氟化物的存在下; 以及将式(I)的卤素取代的2-(氨基亚甲基)-3-氧代丁酸酯进一步转化为卤代甲基取代的吡唑-4-基羧酸及其酯。

    Method for preparing 1,3,4-substituted pyrazol compounds
    56.
    发明申请
    Method for preparing 1,3,4-substituted pyrazol compounds 有权
    制备1,3,4-取代吡唑化合物的方法

    公开(公告)号:US20110172436A1

    公开(公告)日:2011-07-14

    申请号:US12990340

    申请日:2009-05-04

    IPC分类号: C07D231/14 C07C243/10

    摘要: The invention provides an Ethernet bridge or router comprising a network fabric adapted to provide interconnectivity to a plurality of Ethernet ports, each of the Ethernet ports being adapted to receive and/or transmit Ethernet frames, and wherein the Ethernet bridge or router further comprises an encapsulator connected to receive Ethernet Protocol Data Units from the Ethernet ports, wherein the encapsulator is operable to generate a Fabric Protocol Data Unit from a received Ethernet Protocol Data Unit, the Fabric Protocol Data Unit comprising a header portion, and a payload portion which comprises the Ethernet Protocol Data Unit concerned, and wherein the encapsulator is operable to transform Ethernet destination address information from the Ethernet Protocol Data Unit into a routing definition for the network fabric, and to include this routing definition in the header portion of the Fabric Protocol Data Unit. Also provided is a method of data delivery across a network.

    摘要翻译: 本发明提供了一种以太网桥或路由器,其包括适于提供与多个以太网端口的互连性的网络结构,每个以太网端口适于接收和/或发送以太网帧,并且其中所述以太网桥或路由器还包括封装器 连接以从以太网端口接收以太网协议数据单元,其中所述封装器可操作以从接收到的以太网协议数据单元生成结构协议数据单元,所述结构协议数据单元包括报头部分和包括以太网的有效载荷部分 协议数据单元,并且其中所述封装器可操作以将以太网目的地地址信息从以太网协议数据单元转换为所述网络结构的路由定义,并将所述路由定义包括在所述结构协议数据单元的报头部分中。 还提供了一种通过网络进行数据传送的方法。

    Method for the production of substituted 2-aryl malonic acid esters
    57.
    发明申请
    Method for the production of substituted 2-aryl malonic acid esters 审中-公开
    制备取代的2-芳基丙二酸酯的方法

    公开(公告)号:US20100056820A1

    公开(公告)日:2010-03-04

    申请号:US12522211

    申请日:2008-01-21

    IPC分类号: C07C69/34

    摘要: The present invention relates to a process for preparing substituted 2-arylmalonic esters of the general formula I in which R is C1-C6-alkyl or C1-C4-alkoxy-C1-C4-alkyl; Ar is phenyl or a heteroaromatic 5- or 6-membered ring; where each carbon atom present in the radicals mentioned above optionally carries a substituent RA; RA is F, Cl, CN, NO2, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy, etc., or two adjacent substituents RA together with the carbon atoms to which they are attached form a ring; and where a malonic ester is reacted with a base and an aryl bromide in the presence of a copper salt, which comprises employing from 0.1 to 0.65 molar equivalents of the base per molar equivalent of the malonic ester.

    摘要翻译: 本发明涉及制备通式Ⅰ的取代的2-芳基丙二酸酯的方法,其中R是C 1 -C 6 - 烷基或C 1 -C 4 - 烷氧基-C 1 -C 4烷基; Ar是苯基或杂芳族5或6元环; 其中存在于上述基团中的每个碳原子任选地带有取代基RA; RA是F,Cl,CN,NO 2,C 1 -C 4 - 烷基,C 1 -C 4卤代烷基,C 1 -C 4 - 烷氧基,C 1 -C 4 - 卤代烷氧基等,或两个相邻的取代基RA与它们 连接形成环; 并且其中丙二酸酯在铜盐存在下与碱和芳基溴反应,其包括使用每摩尔当量丙二酸酯0.1至0.65摩尔当量的碱。

    Process for preparing 2-(aminomethylidene)-4,4-difluoro-3-oxobutyric esters
    60.
    发明授权
    Process for preparing 2-(aminomethylidene)-4,4-difluoro-3-oxobutyric esters 有权
    制备2-(氨基亚甲基)-4,4-二氟-3-氧代丁酸酯的方法

    公开(公告)号:US08314233B2

    公开(公告)日:2012-11-20

    申请号:US12990359

    申请日:2009-04-30

    摘要: The present invention relates to a process for preparing difluoromethyl-substituted pyrazol-4-ylcarboxylic acids and their esters, 2-(aminomethylidene)-4,4-difluoro-3-oxobutteric esters of the formula (I) in which R1, R2 and R3 independently of one another are C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C3-C10-cycloalkyl or benzyl or NR2R3 is a 5- to 10-membered heterocyclic radical, to a process for preparing compounds of the formula (I) wherein an appropriate 3-aminoacrylic ester is reacted with difluoroacetyl fluoride and to the use of compounds of the formula (I) in the process for preparing difluoromethyl-substituted pyrazol-4-ylcarboxylic acids and their esters.

    摘要翻译: 本发明涉及式(I)的二氟甲基取代的吡唑-4-基羧酸及其酯,2-(氨基亚甲基)-4,4-二氟-3-氧代苦味酯的方法,其中R 1,R 2和 R 3彼此独立地是C 1 -C 6 - 烷基,C 1 -C 6 - 卤代烷基,C 2 -C 6 - 烯基,C 3 -C 10 - 环烷基或苄基或NR 2 R 3是5-至10-元杂环基, 式(I)的化合物,其中适当的3-氨基丙烯酸酯与二氟乙酰氟反应,以及在制备二氟甲基取代的吡唑-4-基羧酸及其酯的方法中使用式(I)的化合物。