Phthalazine derivatives as phosphodiesterase 4-inhibitors
    1.
    发明申请
    Phthalazine derivatives as phosphodiesterase 4-inhibitors 审中-公开
    酞嗪衍生物作为磷酸二酯酶4-抑制剂

    公开(公告)号:US20040043999A1

    公开(公告)日:2004-03-04

    申请号:US10441177

    申请日:2003-05-20

    Abstract: A process for preparing a compound of formula I: 1 wherein G is methylene, ethylene, CONH, amino or a bond; R is H, phenyl or a (C1-4)alkyl group optionally substituted by phenyl; Cy is phenyl or a 5- or 6-membered heterocycle of the group consisting of pyrrole, imidazole, pyrazole, pyrrolidine, pyrroline, imidazoline, imidazolidine, pyrazolidine, pyrazoline, pyridine, pyrazine, pyrimidine, pyridazine, piperazine, piperidine, and triazine, the Cy residue being optionally substituted by one or more substituent(s) selected from the group consisting of keto, nitro, carboxy, fluorine, chlorine, bromine, or iodine; R1 is a (C1-6)alkyl or polyfluoro(C1-6)alkyl group; and R2 is aryl, aryl-(C1-10)-alkyl, (C4-7)cycloalkyl or (C4-7)heterocycle wherein the heteroatom is an oxygen atom.

    Abstract translation: 制备式I化合物的方法:其中G是亚甲基,亚乙基,CONH,氨基或键; R是H,苯基或任选被苯基取代的(C 1-4)烷基; Cy是苯基或由吡咯,咪唑,吡唑,吡咯烷,吡咯啉,咪唑啉,咪唑烷,吡唑烷,吡唑啉,吡啶,吡嗪,嘧啶,哒嗪,哌嗪,哌啶和三嗪组成的组的5-或6-元杂环, Cy残基任选被一个或多个选自酮,硝基,羧基,氟,氯,溴或碘的取代基取代; R1是(C1-6)烷基或多氟(C1-6)烷基; 并且R 2是芳基,芳基 - (C 1-10) - 烷基,(C 4-7)环烷基或(C 4-7)杂环,其中杂原子是氧原子。

    Process for the preparation of (pyridinylidene)-phthalides
    3.
    发明申请
    Process for the preparation of (pyridinylidene)-phthalides 失效
    制备(亚吡啶基) - 酞菁的方法

    公开(公告)号:US20040068117A1

    公开(公告)日:2004-04-08

    申请号:US10671525

    申请日:2003-09-29

    Inventor: Mauro Napoletano

    CPC classification number: C07D405/06

    Abstract: A process for the preparation of phthalazines by preparing intermediate (pyridinylidene)-phthalides starting from 3-oxo-1,3-dihydro-isobenzofuran-1-carboxylic acids and pyridinecarbaldehydes, is described.

    Abstract translation: 描述了从3-氧代-1,3-二氢 - 异苯并呋喃-1-羧酸和吡啶甲醛开始制备中间体(亚吡啶基) - 酞菁的制备酞嗪的方法。

    Process for the preparation of nitroalkenes
    5.
    发明申请
    Process for the preparation of nitroalkenes 审中-公开
    硝基烯烃的制备方法

    公开(公告)号:US20040006248A1

    公开(公告)日:2004-01-08

    申请号:US10311319

    申请日:2002-12-30

    CPC classification number: C07C201/08 C07C2602/28 C07D311/58 C07C205/05

    Abstract: A process for the nitration of conjugated alkenes of formula (I) wherein R, R1, R2, R3 and R4 have the meanings reported in the description, which allows to obtain the corresponding null-nitro-alkenes, characterised in that the nitrating agent is a mixture of an inorganic nitrite and iodine in the presence of an oxidising agent is described. 1

    Abstract translation: 用于硝化式(I)的共轭烯的方法,其中R,R 1,R 2,R 3和R 4具有在说明书中报道的含义,其允许获得相应的β-硝基 - 烯烃,其特征在于硝化剂是 描述了在氧化剂存在下无机亚硝酸盐和碘的混合物。

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