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1. 发明授权

US08153844B2 Process for making 3-substituted 2-amino-5-halobenzamides 有权
标题翻译：制备3-取代的2-氨基-5-卤代苯甲酰胺的方法
公开(公告)号：US08153844B2
公开(公告)日：2012-04-10
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： C07C231/02 , C07C271/28 , C07D265/26
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。

2. 发明申请

US20090306372A1 Process for Making 3-Substituted 2-Amino-5-Halobenzamides 有权
标题翻译： 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。

3. 发明授权

US08871939B2 Method for preparing 2-aminobenzamide derivatives 有权
标题翻译： 2-氨基苯甲酰胺衍生物的制备方法
公开(公告)号：US08871939B2
公开(公告)日：2014-10-28
申请号：US13981919
申请日：2012-01-27
申请人： Sigridur Soley Kristjansdottir , Rafael Shapiro , Matthew Richard Oberholzer
发明人： Sigridur Soley Kristjansdottir , Rafael Shapiro , Matthew Richard Oberholzer
IPC分类号： C07C231/10 , C07D231/14 , C07D401/04
CPC分类号： C07C231/02 , C07C231/10 , C07D231/14 , C07D401/04 , C07C237/30
摘要： A method for preparing a compound of Formula 1 comprising contacting a compound of Formulae 2 and 3 in the presence of a palladium source, a ligand, a base and carbon monoxide wherein R1, R2, X and R3 are as defined in the disclosure. A method for preparing a compound of Formula 5 wherein R1, R2, R3, R4, R5, R6 and Z are as defined in the disclosure, using a compound of Formula 1 characterized by preparing a compound of Formula 1 by the method disclosed above or using a compound of Formula 1 prepared by the method above.
摘要翻译：制备式1化合物的方法，包括在钯源，配体，碱和一氧化碳的存在下使式2和3的化合物接触，其中R 1，R 2，X和R 3如本公开所定义。制备式5化合物的方法，其中R 1，R 2，R 3，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化合物或式使用通过上述方法制备的式1的化合物。

4. 发明申请

US20100280251A1 PROCESS FOR PREPARING 2-AMINO-5-CYANOBENZOIC ACID DERIVATIVES 有权
标题翻译：制备2-氨基-5-氰基苯甲酸衍生物的方法
公开(公告)号：US20100280251A1
公开(公告)日：2010-11-04
申请号：US12516807
申请日：2007-12-18
申请人： Joerg Bruening , Gary David Annis , Martin James Currie , Donald J. Dumas , Rafael Shapiro
发明人： Joerg Bruening , Gary David Annis , Martin James Currie , Donald J. Dumas , Rafael Shapiro
IPC分类号： C07D401/04 , C07C253/32 , C07C231/22 , C07D231/22 , C07D231/12
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。

5. 发明授权

US06489517B1 Process for preparing 3,3′,6,6′-tetraalkyl-2,2′-biphenols and 3,3′,6,6′-tetraalkyl-5,5′-dihalo-2,2′-biphenols 有权
标题翻译：制备3,3'，6,6'-四烷基-2,2'-联苯酚和3,3'，6,6'-四烷基-5,5'-二卤代-2,2'-联苯酚的方法
公开(公告)号：US06489517B1
公开(公告)日：2002-12-03
申请号：US09994098
申请日：2001-11-26
申请人： Rafael Shapiro
发明人： Rafael Shapiro
IPC分类号： C07C3912
CPC分类号： C07C37/00 , C07C37/11 , C07C37/14 , C07C37/50 , C07C37/62 , C07C39/15 , C07C39/28 , C07C39/367 , C07C39/06
摘要： A process for making a compound of the formula I
摘要翻译：制备式的化合物的方法

6. 发明授权

US4904299A Herbicidal N-hydroxy-N'-sulfonylguanidines 失效
标题翻译：除草剂N-羟基-N'-磺酰基胍
公开(公告)号：US4904299A
公开(公告)日：1990-02-27
申请号：US156891
申请日：1988-02-17
申请人： Rafael Shapiro
发明人： Rafael Shapiro
IPC分类号： A01N47/36 , A01N47/42 , A01N47/44 , C07D239/42 , C07D239/46 , C07D239/52 , C07D251/46 , C07D521/00
CPC分类号： C07D239/42 , A01N47/36 , A01N47/42 , A01N47/44 , C07D239/47 , C07D239/52 , C07D251/46 , C07D521/00
摘要： Novel N-hydroxy-N'-sulfonylguanidine compounds are described which possess significant herbicidal and plant growth regulant activity for control of undesired vegetation.
摘要翻译：描述了新的N-羟基-N'-磺酰基胍化合物，其具有显着的除草和植物生长调节活性以控制不希望的植物。

7. 发明授权

US4693744A Herbicidal ortho-(azinyl)-benzenesulfonamides 失效
标题翻译：除草剂邻 - （吖嗪基） - 苯磺酰胺
公开(公告)号：US4693744A
公开(公告)日：1987-09-15
申请号：US858760
申请日：1986-05-02
申请人： Rafael Shapiro
发明人： Rafael Shapiro
IPC分类号： A01N47/36 , C07D213/34 , C07D307/68 , C07D521/00 , C07D401/12
CPC分类号： C07D521/00 , A01N47/36 , C07D213/34 , C07D307/68
摘要： This invention relates to novel ortho-(azinyl)-benzenesulfonamides, such as N[(4-methoxy-6-methylpyrimidin-2-yl)aminocarbonyl]-2-(2-pyridinyl)benzenesulfonamide, and their use as pre-emergent or post-emergent herbicides or plant growth regulants.
摘要翻译：本发明涉及新的邻 - （吖嗪基） - 苯磺酰胺，例如N [（4-甲氧基-6-甲基嘧啶-2-基）氨基羰基] -2-（2-吡啶基）苯甲磺酰胺，及其作为出苗前或出苗后除草剂或植物生长调节剂。

8. 发明授权

US4689070A Herbicidal N-hydroxy-N'-sulfonylguanidines 失效
公开(公告)号：US4689070A
公开(公告)日：1987-08-25
申请号：US736950
申请日：1985-05-22
申请人： Rafael Shapiro
发明人： Rafael Shapiro
IPC分类号： A01N47/36 , A01N47/42 , A01N47/44 , C07D239/42 , C07D239/46 , C07D239/52 , C07D251/46 , C07D521/00
CPC分类号： C07D239/42 , A01N47/36 , A01N47/42 , A01N47/44 , C07D239/47 , C07D239/52 , C07D251/46 , C07D521/00
摘要： Novel N-hydroxy-N'-sulfonylguanidine compounds are described which possess significant herbicidal and plant growth regulant activity for control of undesired vegetation.

9. 发明授权

US4639265A Thiophene or furan herbicides 失效
标题翻译：噻吩或呋喃除草剂
公开(公告)号：US4639265A
公开(公告)日：1987-01-27
申请号：US764617
申请日：1985-08-12
申请人： Rafael Shapiro
发明人： Rafael Shapiro
IPC分类号： A01N47/36 , C07D333/34 , C07D491/048 , C07D491/052 , C07D521/00 , C07D239/70
CPC分类号： C07D521/00 , A01N47/36 , C07D333/34
摘要： Novel thiophenes or furans show herbicidal activity and may also have post- and pre-emergence crop tolerance, especially to corn.
摘要翻译：新的噻吩或呋喃显示出除草活性，也可能具有后期和出苗前的作物耐受性，特别是玉米。

10. 发明授权

US08669277B2 Solid forms of an azocyclic amide 有权
标题翻译：固体形式的杂环酰胺
公开(公告)号：US08669277B2
公开(公告)日：2014-03-11
申请号：US13265138
申请日：2010-04-19
申请人： Matthew Richard Oberholzer , Robert James Pasteris , Rafael Shapiro
发明人： Matthew Richard Oberholzer , Robert James Pasteris , Rafael Shapiro
IPC分类号： A61K31/454 , C07D417/14
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。

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