Synthesis methods and intermediates for the manufacture of rizatriptan
    51.
    发明申请
    Synthesis methods and intermediates for the manufacture of rizatriptan 失效
    合成方法和制造利扎曲坦的中间体

    公开(公告)号:US20070123711A1

    公开(公告)日:2007-05-31

    申请号:US10586958

    申请日:2005-01-27

    IPC分类号: C07D403/02

    摘要: The invention relates to a process for the manufacture of an 1,2,4-triazol-1-yl compound of the formula [A], or a salt thereof, wherein each of R3 and R4 is hydrogen or lower alkyl, said process comprising reacting a hydrazine compound of the formula [B] wherein R is hydrogen or acyl, R2 is hydrogen or a protecting group, are hydrogen or lower alkyl, and R6 is hydrogen or COOR7, or a salt thereof, with a 1,2,4-triazolyl forming reagent. In addition, novel intermediates for the synthesis of the anti-migraine agent Rizatriptan and methods for their synthesis are presented.

    摘要翻译: 本发明涉及一种制备式[A]的1,2,4-三唑-1-基化合物或其盐的方法,其中R 3和R 4各自为氢或低级烷基,所述方法包括 使式[B]的肼化合物其中R是氢或酰基,R2是氢或保护基,是氢或低级烷基,R6是氢或COOR7或其盐与1,2,4 三唑基形成试剂。 此外,还提出了用于合成抗偏头痛药物利扎曲坦的新型中间体及其合成方法。

    Process for the sulfurization of a phosphorus-containing compound
    52.
    发明授权
    Process for the sulfurization of a phosphorus-containing compound 有权
    含磷化合物硫化方法

    公开(公告)号:US07098325B2

    公开(公告)日:2006-08-29

    申请号:US10266027

    申请日:2002-10-07

    摘要: The invention relates to a process for the sulfurization of phosphorus-containing compounds which comprises contacting the phosphorus compound to be sulfurized with a sulfur transfer reagent of formula (I) wherein R1 is aryl which can be substituted by halo, (C1–C6) alkyl or (C1-C6) alkoxy, and R2 is (C1–C6) alkyl, which could also form a cyclic ring together with R1, in a solvent or a mixture of solvents.

    摘要翻译: 本发明涉及含磷化合物的硫化方法,其包括使待硫化的磷化合物与式(I)的硫转移试剂接触,其中R 1是可以被 卤素,(C 1 -C 6 -C 6)烷基或(C 1 -C 6 -C 6)烷氧基,R (C 1 -C 6 -C 6)烷基,其也可以与R 1一起形成环, ,在溶剂或溶剂的混合物中。

    2'-Substituted nucleosides and oligonucleotide derivatives
    53.
    发明申请
    2'-Substituted nucleosides and oligonucleotide derivatives 审中-公开
    2'-取代的核苷和寡核苷酸衍生物

    公开(公告)号:US20050159374A1

    公开(公告)日:2005-07-21

    申请号:US10696488

    申请日:2003-10-29

    CPC分类号: C07H21/00

    摘要: The invention relates to an oligonucleotide derivative which comprises at least one nucleoside building block of the formula (I) The invention furthermore relates to nucleoside building blocks, intermediates and processes for preparing the oligonucleotide derivatives and the nucleoside building blocks. The invention also relates to pharmaceutical compositions and to uses of the oligonucleotide derivatives and the nucleoside building blocks.

    摘要翻译: 本发明涉及包含至少一种式(I)核苷结构单元的寡核苷酸衍生物。本发明还涉及核苷结构单元,中间体和制备寡核苷酸衍生物和核苷结构单元的方法。 本发明还涉及药物组合物以及寡核苷酸衍生物和核苷结构单元的用途。

    5-halo-1,2,3-(1,2-dihydropyrrolo)-4-quinolones
    55.
    发明授权
    5-halo-1,2,3-(1,2-dihydropyrrolo)-4-quinolones 失效
    5-卤代-1,2,3-(1,2-二氢吡咯)-4-喹诺酮类

    公开(公告)号:US4595755A

    公开(公告)日:1986-06-17

    申请号:US759976

    申请日:1985-07-29

    申请人: Pierre Martin

    发明人: Pierre Martin

    IPC分类号: C07D471/06

    CPC分类号: C07D471/06

    摘要: There is described a novel process for producing 1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]-quinolin-4-one (4-lilolidone), usable as fungicide and corresponding to the formula ##STR1## as well as novel 5-halo-1,2,3-(1,2-dihydropyrrolo)-4-quinolones of the formula ##STR2## in which "Hal" is chlorine or bromine, which are formed as intermediates during the process.

    摘要翻译: 描述了用于制备1,2,5,6-四氢-4H-吡咯并[3,2,1-ij] - 喹啉-4-酮(4-二烯醇)的新方法,其可用作杀真菌剂并对应于式 < IMAGE>以及式“IMAGE”的新的5-卤代-1,2,3-(1,2-二氢吡咯并)-4-喹诺酮,其中“Hal”是氯或溴,它们作为中间体形成 的过程。

    5-Haloalkyl-pyridines
    56.
    发明授权
    5-Haloalkyl-pyridines 失效
    5-卤代烷基 - 吡啶

    公开(公告)号:US4577028A

    公开(公告)日:1986-03-18

    申请号:US434433

    申请日:1982-10-14

    摘要: Novel 5-haloalkyl-pyridines suitable for producing pesticidal compositions, particularly insecticides, and corresponding to the formula ##STR1## wherein R is a C.sub.2 -C.sub.10 -alkyl group which is uniformly or nonuniformly substituted by 1 to 21 halogen atoms, and X is halogen;processes for producing them, as well as to the novel starting products and intermediates used or intermediately produced or formed in the production processes.

    摘要翻译: 适用于生产杀虫剂组合物,特别是杀虫剂的新型5-卤代烷基 - 吡啶类化合物,对应于式(Ⅰ)其中R是C2-C10烷基,其被1-22个卤素原子均匀或不均匀地取代,X是卤素 ; 生产方法,以及在生产过程中使用或中间生产或形成的新型起始产品和中间体。

    Process for producing 2,3,5-trichloropyridine,
2,4,4-trichloro-4-formyl-butyronitrile as a novel compound and a
process for producing it
    58.
    发明授权
    Process for producing 2,3,5-trichloropyridine, 2,4,4-trichloro-4-formyl-butyronitrile as a novel compound and a process for producing it 失效
    制备2,3,5-三氯吡啶,2,4,4-三氯-4-甲酰基 - 丁腈作为新化合物的方法及其制备方法

    公开(公告)号:US4245098A

    公开(公告)日:1981-01-13

    申请号:US098017

    申请日:1979-11-28

    IPC分类号: C07C255/17 C07D213/61

    CPC分类号: C07C255/00 C07D213/61

    摘要: A novel process for producing 2,3,5-trichloropyridine is described. The process comprises the addition reaction of trichloroacetaldehyde with acrylonitrile in the presence of a catalyst, and the subsequent cyclization of the intermediately formed 2,4,4-trichloro-4-formylbutyronitrile, with the splitting-off of water, to give 2,3,5-trichloropyridine.2,4,4-Trichloro-4-formylbutyronitrile occurring as an intermediate product in the process according to the invention is a novel compound. It can be produced by the addition reaction of trichloroacetaldehyde with acrylonitrile in the presence of a catalyst.2,3,5-Trichloropyridine can be used as intermediate for the production of herbicidal active substances.

    摘要翻译: 描述了一种制备2,3,5-三氯吡啶的新方法。 该方法包括在催化剂存在下三氯乙醛与丙烯腈的加成反应,随后将中间形成的2,4,4-三氯-4-甲酰基丁腈与水分离,得到2,3 ,5-三氯吡啶。 作为本发明方法中间产物的2,4,4-三氯-4-甲酰基丁腈是一种新型化合物。 它可以通过三氯乙醛与丙烯腈在催化剂存在下的加成反应来制备。 2,3,5-三氯吡啶可用作生产除草活性物质的中间体。

    Process for the preparation of
2-(2',2',2'-trihalogenoethyl)-4-halogenocyclobutan-1-ones
    59.
    发明授权
    Process for the preparation of 2-(2',2',2'-trihalogenoethyl)-4-halogenocyclobutan-1-ones 失效
    制备2-(2',2',2'-三卤代乙基)-4-卤代环丁烷-1-酮的方法

    公开(公告)号:US4242278A

    公开(公告)日:1980-12-30

    申请号:US948126

    申请日:1978-10-03

    摘要: A process for the preparation of 2-(2',2',2',-trihalogenoethyl)-4-halogenocyclobutan-1-ones of the formula ##STR1## in which one of the radicals R.sub.1 and R.sub.2 is methyl and the other is hydrogen or methyl, or R.sub.1 and R.sub.2 together are an alkylene group having 2 to 4 carbon atoms, and X and Y are each chlorine or bromine, comprising reacting a 2,4,4,4-tetrahalogenobutyric acid chloride in the presence of an organic base with an ethylene compound which is disubstituted in 1-position by the radicals R.sub.1 and R.sub.2, as defined above, to form a 2-(2',2',2'-trihalogenoethyl)-2-halogenocyclobutan-1-one and then rearranging the latter, in the presence of a catalyst, into a 2-(2',2',2'-trihalogenoethyl)-4-halogenocyclobutan-1-one of the above formula; said 2-(2',2',2'-trihalogenoethyl)-4-halogenocyclobutan-1-ones being valuable intermediates for the preparation of 2-(2',2'-dihalogenovinyl)-cyclopropanecarboxylic acid and its insecticidally active esters; as well as the 2-(2',2',2'-trihalogenoethyl)-4-halogenocyclobutan-1-ones of the above formula and the intermediates utilized for their preparation.

    摘要翻译: 一种制备式(IMAGE)的2-(2',2',2', - 三卤代乙基)-4-卤代环丁烷-1-酮的方法,其中R 1和R 2之一是甲基,另一个是 氢或甲基,或R 1和R 2一起是具有2至4个碳原子的亚烷基,X和Y各自为氯或溴,包括在有机物存在下使2,4,4,4-四卤代丁酰氯反应 与如上定义的基团R 1和R 2在1位被二取代的亚乙基化合物反应形成2-(2',2',2'-三卤代乙基)-2-卤代环丁烷-1-酮,然后 在催化剂存在下将其重新排列成上式的2-(2',2',2'-三卤代乙基)-4-卤代环丁烷-1-酮; 所述2-(2',2',2'-三卤代乙基)-4-卤代环丁烷-1-酮是制备2-(2',2'-二卤代乙酰基) - 环丙烷羧酸及其杀虫活性酯的有价值的中间体; 以及上述式的2-(2',2',2'-三卤代乙基)-4-卤代环丁烷-1-酮和用于其制备的中间体。