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    SOLID FORMS OF AN AZOCYCLIC AMIDE
    1.
    发明申请
    SOLID FORMS OF AN AZOCYCLIC AMIDE 有权
    AZOCYCLIC酰胺的固体形式

    公开(公告)号：US20120034315A1

    公开(公告)日：2012-02-09

    申请号：US13265138

    申请日：2010-04-19

    申请人： Mary Ann Hanagan ,  Matthew Richard Oberholzer ,  Robert James Pasteris ,  Rafael Shapiro

    发明人： Mary Ann Hanagan ,  Matthew Richard Oberholzer ,  Robert James Pasteris ,  Rafael Shapiro

    IPC分类号： A01N59/20 ,  A61K31/454 ,  A01N43/90 ,  A01N43/54 ,  A01P7/04 ,  A01N57/12 ,  A01N57/10 ,  A01N43/42 ,  A01P3/00 ,  C07D417/14 ,  A01N55/10

    CPC分类号： C07D417/14 ,  A01N43/653 ,  A01N43/80 ,  A01N43/84 ,  A01N57/12 ,  A01N59/20

    摘要： Disclosed are solid forms of 1-[4-[4-[5-(2,6-difluorophenyl)-4,5-dihydro-3-isoxazolyl]-2-thiazolyl]-1-piperidinyl]-2-[5-methyl-3-(trifluoromethyl)-1H-pyrazol-1-yl]ethanone (Compound 1). Methods for the preparation of solid forms of Compound 1 and for the conversion of one solid form of Compound 1 into another are disclosed.Disclosed are fungicidal compositions comprising a fungicidally effective amount of a solid form of Compound 1 and at least one additional component selected from the group consisting of surfactants, solid diluents and liquid carriers. Compositions comprising a mixture of a solid form of Compound 1 and at least one other fungicide or insecticide are also disclosed.Also disclosed are methods for controlling plant diseases caused by fungal plant pathogens comprising applying to a plant or portion thereof, or to a plant seed, a fungicidally effective amount of a solid form of Compound 1.

    摘要翻译： 公开了1- [4- [4- [5-（2,6-二氟苯基）-4,5-二氢-3-异恶唑基] -2-噻唑基] -1-哌啶基] -2- [5- （三氟甲基）-1H-吡唑-1-基]乙酮（化合物1）。 公开了制备化合物1的固体形式和将一种固体形式的化合物1转化成另一种的方法。 公开了包含杀真菌有效量的固体形式的化合物1和至少一种选自表面活性剂，固体稀释剂和液体载体的另外的组分的杀真菌组合物。 还公开了包含固体形式的化合物1和至少一种其它杀真菌剂或杀虫剂的混合物的组合物。 还公开了用于控制由真菌植物病原体引起的植物疾病的方法，包括向植物或其部分或植物种子施用杀真菌有效量的化合物1的固体形式。

    Process for preparing 2-amino-5-cyanobenzoic acid derivatives
    2.
    发明授权
    Process for preparing 2-amino-5-cyanobenzoic acid derivatives 有权
    制备2-氨基-5-氰基苯甲酸衍生物的方法

    公开(公告)号：US08049029B2

    公开(公告)日：2011-11-01

    申请号：US12516807

    申请日：2007-12-18

    申请人： Joerg Bruening ,  Gary David Annis ,  Donald J Dumas ,  Rafael Shapiro

    发明人： Joerg Bruening ,  Gary David Annis ,  Donald J Dumas ,  Rafael Shapiro

    IPC分类号： C07C253/00

    CPC分类号： C07C253/14 ,  C07C231/12 ,  C07C233/65 ,  C07C255/58

    摘要： Disclosed is a method for preparing a compound of Formula 1 comprising contacting a compound of Formula 2 with a metal cyanide reagent, a copper(I) salt reagent, an iodide salt reagent and at least one compound of Formula 3 wherein R1 is NHR3 or OR4; R2 is CH3 or Cl; R3 is H, C1-C4 alkyl, cyclopropyl, cyclopropylcyclopropyl, cyclopropylmethyl or methylcyclopropyl; R4 is H or C1-C4 alkyl; Y is Br or Cl; X is NR13 or O; n is 0 or 1; and R5, R6, R7, R8, R9, R10, R11, R12 and R13 are as defined in the disclosure. Also disclosed is a method for preparing a compound of Formula 2 wherein Y is Br and R1 is NHR3 comprising introducing a gas containing bromine into a liquid containing a compound of Formula 4, and further disclosed is a method for preparing a compound of Formula 5 wherein R14, R15, R16 and Z are as defined in the disclosure using a compound of Formula 1 characterized by preparing the compound of Formula 1 by the method disclosed above.

    摘要翻译： 公开了一种制备式1化合物的方法，包括使式2化合物与金属氰化物试剂，铜（I）盐试剂，碘化物盐试剂和至少一种式3化合物（其中R1是NHR3或OR4）接触 ; R2是CH3或Cl; R3是H，C1-C4烷基，环丙基，环丙基环丙基，环丙基甲基或甲基环丙基; R4是H或C1-C4烷基; Y为Br或Cl; X为NR 13或O; n为0或1; 并且R5，R6，R7，R8，R9，R10，R11，R12和R13如本公开所定义。 还公开了制备式2化合物的方法，其中Y是Br，R 1是NHR 3，包括将含溴的气体引入含有式4化合物的液体中，并且还公开了制备式5化合物的方法，其中 R14，R15，R16和Z如本公开中所定义，使用式1的化合物，其特征在于通过上述方法制备式1的化合物。

    Process for Making 3-Substituted 2-Amino-5-Halobenzamides
    3.
    发明申请
    Process for Making 3-Substituted 2-Amino-5-Halobenzamides 有权
    3-取代的2-氨基-5-卤代苯甲酰胺的制备方法

    公开(公告)号：US20090306372A1

    公开(公告)日：2009-12-10

    申请号：US12373651

    申请日：2007-06-27

    申请人： Richard F. Davis ,  Rafael Shapiro ,  Eric G. Taylor

    发明人： Richard F. Davis ,  Rafael Shapiro ,  Eric G. Taylor

    IPC分类号： C07C231/10 ,  C07D265/26 ,  C07D401/04 ,  C07D231/20 ,  C07D231/14 ,  C07C271/06 ,  C07C271/10

    CPC分类号： C07D401/04 ,  C07C231/02 ,  C07C271/28 ,  C07D231/16 ,  C07D265/26 ,  C07C237/30

    摘要： Disclosed is a method for preparing a compound of Formula 1 by contacting compound of Formula 2 with R1—NH2 in the presence of a carboxylic acid and a method for preparing a compound of Formula 2 by contacting a compound of Formula 4 with phosphorus tribromide. wherein R1 is H, C1-C4 alkyl, cyclopropyl, cyclopropylmethyl or methylcyclopropyl; R2 is CH3 or Cl; R3 is C1-C6 alkyl or C3-C6 alkenyl, each optionally substituted with up to 3 halogen and up to 1 phenyl; and X is Cl or Br. Also disclosed is a method for preparing a compound of Formula 5 wherein R4, R5, R6 and Z are as defined in the disclosure, using a compound of Formula 1 that is characterized by preparing the compound of Formula 1 by the method above.

    摘要翻译： 公开了通过在羧酸存在下使式2的化合物与R 1 -NH 2接触来制备式1化合物的方法和通过使式4的化合物与三溴化磷接触来制备式2的化合物的方法。 其中R1是H，C1-C4烷基，环丙基，环丙基甲基或甲基环丙基; R2是CH3或Cl; R 3是C 1 -C 6烷基或C 3 -C 6烯基，各自任选被至多3个卤素和至多1个苯基取代; X为Cl或Br。 还公开了制备式5化合物的方法，其中R 4，R 5，R 6和Z如本公开所定义，使用式1化合物，其特征在于通过上述方法制备式1化合物。

    Process for the manufacture of 2,3-dichloropyridine
    5.
    发明申请
    Process for the manufacture of 2,3-dichloropyridine 审中-公开
    2,3-二氯吡啶的制备方法

    公开(公告)号：US20070161797A1

    公开(公告)日：2007-07-12

    申请号：US10583635

    申请日：2005-01-21

    申请人： Rafael Shapiro

    发明人： Rafael Shapiro

    IPC分类号： C07D213/61

    CPC分类号： C07D213/61 ,  C07D213/73 ,  C07D213/82

    摘要： A method for preparing 2,3-dichloropyridine is disclosed in which 3-amino-2-chloropyridine is contacted with an alkali metal nitrite in the presence of aqueous hydrochloric acid to form a diazonium salt; and the diazonium salt is subsequently decomposed in the presence of copper catalyst wherein at least about 50% of the copper is the copper(II) oxidation state.

    摘要翻译： 公开了一种制备2,3-二氯吡啶的方法，其中3-氨基-2-氯吡啶与碱金属亚硝酸盐在盐酸水溶液的存在下接触以形成重氮盐; 随后在铜催化剂存在下分解重氮盐，其中至少约50％的铜是铜（II）氧化态。