Process for the preparation of substituted heteroaromatics
    2.
    发明申请
    Process for the preparation of substituted heteroaromatics 有权
    制备取代杂芳族化合物的方法

    公开(公告)号:US20100217015A1

    公开(公告)日:2010-08-26

    申请号:US12663536

    申请日:2008-05-27

    IPC分类号: C07D333/10

    CPC分类号: C07D333/08

    摘要: A process is described for the preparation of substituted heteroaromatics of the general formula (I) where X is oxygen, sulphur or NR5 where R5 is hydrogen, C1-C20-alkyl or C5-C6-aryl and R4 is C1-C20-alkyl, C5-C6-aryl or heteroaryl, R1, R2, R3 is hydrogen, halogen, C1-C20-alkyl, C5-C6-aryl or heteroaryl, by reaction A) of a halogenated heteroaromatic of the general formula (II) where X has the meaning given for formula (I) and R6 is bromine, iodine or chlorine and R1, R2 and R3 have the meaning given for formula (I), with a Grignard reagent of the general formula (III) R4MgHal  (III) where R4 has the meaning given for formula (I) and Hal is bromine, iodine or chlorine or B) reaction of the halogenated heteroaromatics of the formula (II) with magnesium firstly to give a Grignard compound of the general formula (IIIa) where Hal is bromine, iodine or chlorine and X and R1, R2 and R3 have the meaning given for formula (I), and further reaction with a halogenated compound of the general formula (IV) R4Hal  (IV) where R4 has the meaning given for formula (I) and Hal is bromine, iodine or chlorine, where the reactions A) or B) are in each case carried out in the presence of an Ni or Pd catalyst, characterized in that the process is carried out in the presence of cycloalkyl alkyl ether as solvent and optionally a further solvent. Likewise described is the use of cycloalkyl alkyl ethers, in particular cyclopentyl methyl ether, in the Kumada reaction for the preparation of substituted heteroaromatics, in particular substituted thiophenes.

    摘要翻译: 描述了制备通式(I)的取代杂芳族化合物的方法,其中X是氧,硫或NR 5,其中R 5是氢,C 1 -C 20 - 烷基或C 5 -C 6 - 芳基,R 4是C 1 -C 20烷基, C 2 -C 6 - 芳基或杂芳基,R 1,R 2,R 3是氢,卤素,C 1 -C 20烷基,C 5 -C 6 - 芳基或杂芳基,通过反应A)通式(II)的卤代杂芳基,其中X具有 对于式(I)和R6给出的含义是溴,碘或氯,并且R 1,R 2和R 3具有式(I)给出的含义,通式(III)的格利雅试剂R4MgHal(III)其中R4具有 式(I)给出的含义和Hal是溴,碘或氯或B)式(II)的卤化杂芳族化合物与镁的反应首先得到通式(IIIa)的格利雅化合物,其中Hal是溴, 碘或氯,X和R 1,R 2和R 3具有式(I)给出的含义,并进一步与本发明的卤代化合物反应 式(IV)R4Hal(IV)其中R4具有式(I)给出的含义,Hal是溴,碘或氯,其中反应A)或B)在每种情况下在Ni或 Pd催化剂,其特征在于该方法在环烷基烷基醚作为溶剂和任选的另外的溶剂的存在下进行。 同样地描述了在Kumada反应中使用环烷基烷基醚,特别是环戊基甲基醚来制备取代的杂芳族化合物,特别是取代的噻吩。

    Process for preparing halogen-substituted dibenzyl alcohols, these halogen-substituted dibenzyl alcohols and their use
    5.
    发明授权
    Process for preparing halogen-substituted dibenzyl alcohols, these halogen-substituted dibenzyl alcohols and their use 失效
    制备卤素取代的二苄醇,这些卤素取代的二苄醇及其用途的方法

    公开(公告)号:US06759558B2

    公开(公告)日:2004-07-06

    申请号:US10117523

    申请日:2002-04-05

    申请人: Lars Rodefeld

    发明人: Lars Rodefeld

    IPC分类号: C07C3328

    CPC分类号: C07C33/46 C07C29/147

    摘要: A novel process allows a simple preparation of highly pure halogen-substituted dibenzyl alcohols by reduction of the corresponding halogen-substituted terephthalic acids and reaction with an alkylating agent, sulfuric acid, alkyl- or arylsulfonic acids. The highly pure halogen-substituted dibenzyl alcohols obtained are suitable in particular for preparing pharmaceutically or agrochemically active compounds.

    摘要翻译: 一种新方法可以通过还原相应的卤素取代的对苯二甲酸和与烷基化剂,硫酸,烷基 - 或芳基磺酸反应来简单地制备高纯度卤代 - 取代的二苄醇。 获得的高纯度卤素取代的二苄醇特别适用于制备药学上或农业化学活性化合物。

    Method for producing 2,3,5,6-tetrahalogen-xylyidene compounds
    7.
    发明授权
    Method for producing 2,3,5,6-tetrahalogen-xylyidene compounds 失效
    制备2,3,5,6-四卤代 - 亚二甲基化合物的方法

    公开(公告)号:US06753444B2

    公开(公告)日:2004-06-22

    申请号:US10181997

    申请日:2002-07-24

    IPC分类号: C07C6976

    CPC分类号: C07C17/093

    摘要: The invention relates to a process for preparing 2,3,5,6-tetrahaloxylylidene compounds of formula (I) where each Hal is independently fluorine or chlorine, and X is fluorine, chlorine, bromine, —O—R, or —O—C(═O)R, where R is hydrogen, a straight-chain or branched C1-C12-alkyl- or a C6-C14-aryl radical, by reacting 2,3,5,6-tetrahaloxylylidenediamines of formula (II) with an alkyl nitrite and/or nitrous acid in HX as a solvent.

    摘要翻译: 本发明涉及一种制备式(I)的2,3,5,6-四卤氧基亚甲基化合物的方法,其中每个Hal独立地为氟或氯,X为氟,氯,溴,-OR或-OC(= O )R,其中R是氢,直链或支链C 1 -C 12 - 烷基 - 或C 6 -C 14 - 芳基,通过使式(II)的2,3,5,6-四烷氧基亚磺酰胺与亚硝酸烷基酯反应,以及 /或HX中的亚硝酸作为溶剂。

    Method for preparing methyl carbazate
    9.
    发明授权
    Method for preparing methyl carbazate 有权
    制备甲基肼基甲酸酯的方法

    公开(公告)号:US06465678B1

    公开(公告)日:2002-10-15

    申请号:US09889813

    申请日:2001-07-20

    IPC分类号: C07C22900

    CPC分类号: C07C281/02

    摘要: Methyl carbazate which is particularly pure and has a particularly low tendency toward discoloration is obtained from hydrazine and dimethyl carbonate if the two reactants are metered simultaneously into an initially introduced first solvent at from −20 to +30° C., the solvent and low-boiling components are then distilled off under reduced pressure, and then either a second solvent is added to the crude methyl carbazate present and this solvent is distilled off under reduced pressure or an inert gas is passed through the crude methyl carbazate present.

    摘要翻译: 如果两个反应物在-20至+ 30℃下同时计量到初始引入的第一溶剂中,则可从肼和碳酸二甲酯得到特别纯的具有特别低的变色趋势的肼基甲酸甲酯, 然后在减压下蒸馏沸腾的组分,然后将第二溶剂加入到存在的粗甲基肼基甲酸酯中,并在减压下蒸馏掉该溶剂,或使惰性气体通过存在的粗甲基肼基甲酸酯。