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    POLYMORPHS OF N-MALONYL-BIS(N`-METHYL-N`-THIOBENZOYLHYDRAZIDE)
    4.
    发明申请
    POLYMORPHS OF N-MALONYL-BIS(N`-METHYL-N`-THIOBENZOYLHYDRAZIDE) 审中-公开
    N-马来酰亚胺（N，N'-甲基-N'-噻唑烷基硫化物）的聚合物

    公开(公告)号：US20140350115A1

    公开(公告)日：2014-11-27

    申请号：US14165448

    申请日：2014-01-27

    Applicant: SYNTA PHARMACEUTICALS CORP.

    Inventor： Elena Kostik ,  Lijun Sun ,  Joanna Dziewiszek ,  Jun Y. Choi

    IPC: C07C327/56

    CPC classification number: C07C327/56 ,  C07B2200/13

    Abstract: At least 70% by weight of Compound 1 is the single crystalline form, Form A, Form C, or Form D, of the compound. A pharmaceutical composition comprises a pharmaceutically acceptable carrier or diluent, and compound 1, wherein at least 70% by weight of the compound is the single crystalline form, Form A, Form C, or Form D, of the compound. A method of treating a subject with cancer comprises administering to the subject an effective amount of compound 1 or the pharmaceutical composition.

    Abstract translation: 化合物1的至少70重量％是化合物的单晶形式，形式A，形式C或形式D. 药物组合物包含药学上可接受的载体或稀释剂和化合物1，其中至少70重量％的化合物是化合物的单晶形式，形式A，形式C或形式D. 用癌症治疗受试者的方法包括向受试者施用有效量的化合物1或药物组合物。

    Insecticidal N'-substituted-N,N'-diacylhydrazines
    5.
    发明授权
    Insecticidal N'-substituted-N,N'-diacylhydrazines 失效
    杀虫N'取代-N，N'-二酰基肼

    公开(公告)号：US5530028A

    公开(公告)日：1996-06-25

    申请号：US129549

    申请日：1993-09-29

    Applicant: Zev Lidert ,  Dat P. Le ,  Robert E. Hormann ,  Thomas R. Opie

    Inventor： Zev Lidert ,  Dat P. Le ,  Robert E. Hormann ,  Thomas R. Opie

    IPC: A01N37/28 ,  A01N33/00 ,  A01N37/40 ,  A01N43/30 ,  A01N43/32 ,  C07C243/38 ,  C07C251/86 ,  C07C255/24 ,  C07C275/28 ,  C07C311/51 ,  C07C323/48 ,  C07C327/56 ,  C07D207/34 ,  C07D213/54 ,  C07D213/87 ,  C07D241/24 ,  C07D303/38 ,  C07D307/58 ,  C07D307/68 ,  C07D307/79 ,  C07D311/58 ,  C07D317/50 ,  C07D317/68 ,  C07D319/18 ,  C07D321/10 ,  C07D333/38 ,  A01N33/26 ,  C07C243/16

    CPC classification number: C07D213/54 ,  A01N37/40 ,  A01N43/30 ,  A01N43/32 ,  C07C243/38 ,  C07C251/86 ,  C07C255/24 ,  C07C275/28 ,  C07C311/51 ,  C07C323/48 ,  C07C327/56 ,  C07D207/34 ,  C07D213/87 ,  C07D241/24 ,  C07D303/38 ,  C07D307/58 ,  C07D307/68 ,  C07D317/68 ,  C07D319/18 ,  C07D333/38 ,  C07C2101/04 ,  C07C2101/14 ,  C07C2101/16 ,  C07C2102/10

    Abstract: Insecticidal compounds having the formula N-(2-R.sup.a -3-R.sup.b -4-R.sup.h -benzoyl)-N'-(2-R.sup.c -3-R.sup.d -4-R.sup.e -5-R.sup.f -benzoyl)-N'-R.sup.g -hydrazine wherein R.sup.a is a halo or lower alkyl; R.sup. b is lower alkoxy, optionally substituted with halo (preferably fluoro); R.sup.c is selected from hydrogen, halo, lower alkyl, lower alkoxy, lower alkoxy lower alkyl, and nitro; R.sup.d, R.sup.e and R.sup.f are each independently selected from hydrogen, bromo, chloro, fluoro, lower alkyl, lower alkoxy, and lower alkoxy lower alkyl; R.sub.g is a (C.sub.4 -C.sub.6)alkyl; R.sup.h is hydrogen, lower alkoxy, lower alkyl, or when taken together with R.sup.b is methylenedioxy (--OCH.sub.2 O--), 1,2-ethylenedioxy (--OCH.sub.2 CH.sub.2 O--), 1,2-ethyleneoxy (--CH.sub.2 CH.sub.2 O--) or 1,3-propyleneoxy (--CH.sub.2 CH.sub.2 CH.sub.2 O--) wherein an oxo atom is located at the R.sup.b position; and the substituents R.sup.c and R.sup.d, or R.sup.d and R.sup.e, or R.sup.e and R.sup.f when taken together can be methylenedioxy or 1,2-ethylenedioxy as well as compositions comprising an agronomically acceptable carrier and an insecticidally effective amount of such compounds; and methods of using such compounds and compositions.Also, methods for the production of the compounds and their intermediates, which methods comprise either admixing a 3-amino-2-(substituted)-benzoic acid, sodium nitrite and methanol under acidic conditions or admixing a 3,4-fused heterocyclic benzoic acid and an alkyl lithium reagent followed by subsequent reaction with an electrophilic reagent.

    Abstract translation: 具有式N-（2-Ra-3-Rb-4-Rh-benzoyl）-N' - （2-Rc-3-Rd-4-Re-5-Rf-benzoyl）-N'-Rg的杀虫化合物 肼，其中R a是卤素或低级烷基; Rb是低级烷氧基，任选被卤素（优选氟）取代; Rc选自氢，卤素，低级烷基，低级烷氧基，低级烷氧基低级烷基和硝基; Rd，Re和Rf各自独立地选自氢，溴，氯，氟，低级烷基，低级烷氧基和低级烷氧基低级烷基; R g是（C 4 -C 6）烷基; 当R 2为氢时，低级烷氧基，低级烷基，或与Rb一起与亚甲二氧基（-OCH 2 O-），1,2-亚乙二氧基（-OCH 2 CH 2 O-），1,2-亚乙基氧基（-CH 2 CH 2 O-） 丙氧基（-CH 2 CH 2 CH 2 O-），其中氧原子位于Rb位; 并且取代基R c和R d，或R d和R Re或Re和R f一起可以是亚甲二氧基或1,2-亚乙二氧基，以及包含农学上可接受的载体和杀虫有效量的这些化合物的组合物; 以及使用这些化合物和组合物的方法。 另外，制备化合物及其中间体的方法，该方法包括在酸性条件下混合3-氨基-2-（取代的） - 苯甲酸，亚硝酸钠和甲醇，或将3,4-稠合的杂环苯甲酸 和烷基锂试剂，随后与亲电试剂反应。

    Production of thiocarbohydrazide on a commercial scale
    10.
    发明授权
    Production of thiocarbohydrazide on a commercial scale 失效
    以商业规模生产硫代碳酰肼

    公开(公告)号：US4294985A

    公开(公告)日：1981-10-13

    申请号：US48856

    申请日：1979-06-15

    Applicant: Gunther Cramm ,  Karl H. Blocher

    Inventor： Gunther Cramm ,  Karl H. Blocher

    IPC: C07C327/56 ,  C01B20060101 ,  C07C20060101 ,  C07C67/00 ,  C07C325/00 ,  C07C335/40 ,  C07C337/06 ,  C07C159/00

    CPC classification number: C07C337/06

    Abstract: In the production of thiocarbohydrazide by reacting hydrazine hydrate with carbon disulphide in the presence of water to form in a first stage hydrazinium dithiocarbazinate, subsequently thermally decomposing the hydrazinium dithiocarbazinate in a second stage to form thiocarbohydrazide, and recovering the thiocarbohydrazide from the reaction medium, the improvement which comprises effecting the entire reaction in the mother liquor of a preceding batch, carrying out the first reaction stage at a temperature between about 25.degree. C. and 45.degree. C., with injection of carbon disulphide below the surface of the reaction mixture; carrying out the second stage at about 62.degree. to 65.degree. C. without prior isolation of the intermediate product; filtering off the thiocarbohydrazide formed after cooling, separating the amount of mother liquor in excess of that required for the next batch, and feeding the balance of the mother liquor to the next batch. The excess mother liquor not required for the next batch is heated to about 70.degree. to 75.degree. C., and after separating off the thiocarbohydrazide, the remaining mother liquor is subjected to combustion.

    Abstract translation: 在硫代碳酰肼的制备中，通过在水存在下使水合肼与二硫化碳反应，在第一阶段中形成二硫代肼基肼，然后在第二阶段热分解二硫代肼基肼，形成硫代碳酰肼，并从反应介质中回收硫代碳酰肼， 其包括进行前一批次的母液中的整个反应，在约25℃至45℃的温度下进行第一反应阶段，在反应混合物的表面下注入二硫化碳; 在大约62°至65℃进行第二阶段，而不预先分离中间产物; 过滤冷却后形成的硫代碳酰肼，将母液的量分离超过下一批所需的母液量，并将母液的余量送入下一批。 将下一批不需要的过量母液加热至约70℃至75℃，分离硫代碳酰肼后，将剩余的母液进行燃烧。

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