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31. 发明授权

US07071365B2 3-alkylated-5,5′,6,6′, 7, 7′, 8, 8′—octahydro-2, 2′-binaphthols and 3, 3′-dialkylated- 5, 5′, 6, 6′, 7, 7′, 8, 8′-octahydro—2, 2′-binaphthols and processes for making 失效
标题翻译： 3-烷基化-5,5'，6,6'，7,7'，8,8'-八氢-2,2'-联萘酚和3,3'-二烷基化-5,5'，6,6' 7,7'，8,8'-八氢-2,2'-联萘酚和制备方法
公开(公告)号：US07071365B2
公开(公告)日：2006-07-04
申请号：US11103044
申请日：2005-04-11
申请人： Helen S. M. Lu , Weiming Qiu , Rafael Shapiro
发明人： Helen S. M. Lu , Weiming Qiu , Rafael Shapiro
IPC分类号： C07C39/12
CPC分类号： C07C39/17 , C07C37/11 , C07C37/14 , C07C37/16 , C07C37/18 , C07C2601/10 , C07C2602/10
摘要： The compositions 3-alkylated-5,5′,6,6′,7,7′,8,8′-octahydro-2,2′-binaphthol and 3,3′-dialkylated-5,5′,6,6′,7,7′,8,8′-octahydro-2,2′-binaphthol are disclosed, as well as various processes for making them, all involving the alkylation of 5,5′,6,6′,7,7′,8,8′-octahydro-2,2′-binaphthol.
摘要翻译：组合物3-烷基化-5,5'，6,6'，7,7'，8,8'-八氢-2,2'-联萘酚和3,3'-二烷基化-5,5'，6,6 '，7,7'，8,8'-八氢-2,2'-联萘酚，以及制备它们的各种方法，所有方法涉及5,5'，6,6'，7,7 '，8,8'-八氢-2,2'-联萘酚。

32. 发明授权

US06080856A Preparation of arthropodicidal oxadiazines 有权
标题翻译：节肢动物毒素恶二嗪的制备
公开(公告)号：US06080856A
公开(公告)日：2000-06-27
申请号：US422631
申请日：1999-10-21
申请人： Gary David Annis , Stephen Frederick McCann , Rafael Shapiro
发明人： Gary David Annis , Stephen Frederick McCann , Rafael Shapiro
IPC分类号： C07C63/68 , C07C65/21 , C07C69/757 , C07C69/76 , C07C69/92 , C07C271/66 , C07C281/04 , C07D273/04
CPC分类号： C07C63/68 , C07C271/66 , C07C281/04 , C07C65/21 , C07C69/757 , C07C69/76 , C07C69/92 , C07D273/04
摘要： A method for making arthropodicidal oxadiazines and intermediates which are racemic or enantiomerically enriched at their chiral center, the method for making the oxadiazines comprising reaction of an intermediate selected from ##STR1## wherein: R.sup.1 is F, Cl, or C.sub.1 -C.sub.3 fluoroalkoxy,R.sup.2 is C.sub.1 -C.sub.3 alkyl, andR.sup.4 is H or CO.sub.2 CH.sub.2 (C.sub.6 H.sub.5).as well as certain selected intermediates including those depicted above, and methods of making them.
摘要翻译：一种在其手性中心进行外消旋或对映体富集的杀虫毒素恶二嗪和中间体的方法，所述制备所述恶二嗪的方法包括选自以下的中间体：R 1为F，Cl或C 1 -C 3氟烷氧基，R 2为C1- C3烷基，R4是H或CO2CH2（C6H5）。以及某些所选择的中间体，包括上述那些，以及制备它们的方法。

33. 发明授权

US4806142A Herbicidal pyrimidine sulfonylureas 失效
标题翻译：除草嘧啶磺酰脲类
公开(公告)号：US4806142A
公开(公告)日：1989-02-21
申请号：US896091
申请日：1986-08-13
申请人： Rafael Shapiro
发明人： Rafael Shapiro
IPC分类号： A01N47/36 , C07D239/42 , C07D405/12 , C07D521/00 , A01N43/54 , A01N43/66 , C07D239/28 , C07D251/46
CPC分类号： C07D239/42 , A01N47/36 , C07D405/12 , C07D521/00
摘要： Certain substituted pyrimidine sulfonylureas, such as 3-[[[-(4-dimethoxymethyl)-6-methylpyrimidin-2-yl]aminocarbonyl]aminosulfonyl]-2-thiophenecarboxylic acid, methyl ester, are selective pre-emergence and/or post-emergence herbicides.
摘要翻译：某些取代的嘧啶磺酰脲，例如3 - [[[ - （4-二甲氧基甲基）-6-甲基嘧啶-2-基]氨基羰基]氨基磺酰基] -2-噻吩甲酸甲酯是选择性芽前和/ 发芽除草剂。

34. 发明授权

US4723988A Herbicidal thiophenesulfonamides 失效
标题翻译：除草噻吩磺酰胺
公开(公告)号：US4723988A
公开(公告)日：1988-02-09
申请号：US031286
申请日：1987-03-27
申请人： Rafael Shapiro
发明人： Rafael Shapiro
IPC分类号： A01N47/36 , C07D401/04 , C07D413/04 , C07D521/00 , C07D401/14 , A01N43/66 , A01N43/70 , C07D409/14
CPC分类号： C07D521/00 , A01N47/36 , C07D401/04 , C07D413/04
摘要： Thiophenesulfonamides such as N-[(4,6-dimethylpyrimidin-2-yl)aminocarbonyl]-3-(isoxazol-3-yl)-2-thiophenesulfonamide are useful as herbicides and plant growth regulants.
摘要翻译：噻吩磺酰胺如N - [（4,6-二甲基嘧啶-2-基）氨基羰基] -3-（异恶唑-3-基）-2-硫代苯磺酰胺可用作除草剂和植物生长调节剂。

35. 发明授权

US4684393A Herbicidal thiophenesulfonamides 失效
公开(公告)号：US4684393A
公开(公告)日：1987-08-04
申请号：US724835
申请日：1985-04-23
申请人： Rafael Shapiro
发明人： Rafael Shapiro
IPC分类号： A01N47/36 , C07D401/04 , C07D413/04 , C07D521/00 , C07D409/14 , C07D411/14 , C07D417/14
CPC分类号： C07D521/00 , A01N47/36 , C07D401/04 , C07D413/04
摘要： Thiophenesulfonamides such as N-[(4,6-dimethylpyrimidin-2-yl)aminocarbonyl]-3-(isoxazol-3-yl)-2-thiophenesulfonamide are useful as herbicides and plant growth regulants.

36. 发明授权

US4629494A Herbicidal sulfonamides 失效
标题翻译：除草磺酰胺
公开(公告)号：US4629494A
公开(公告)日：1986-12-16
申请号：US723450
申请日：1985-04-15
申请人： Rafael Shapiro
发明人： Rafael Shapiro
IPC分类号： A01N47/36 , C07D239/42 , C07D405/12 , C07D521/00 , A01N43/08 , A01N43/10 , A01N43/54 , A01N43/66 , C07D239/69 , C07D251/12
CPC分类号： C07D239/42 , A01N47/36 , C07D405/12 , C07D521/00
摘要： Certain substituted pyrimidine sulfonylureas, such as 3-[[[(4-(dimethoxymethyl)-6-methylpyrimidin-2-yl]aminocarbonyl]aminosulfonyl]-2-thiophenecarboxylic acid, methyl ester, are selective pre-emergence and/or post-emergence herbicides.
摘要翻译：某些取代的嘧啶磺酰脲如3 - [[[（4-（二甲氧基甲基）-6-甲基嘧啶-2-基]氨基羰基]氨基磺酰基] -2-噻吩羧酸甲酯是选择性芽前和/ 发芽除草剂。

37. 发明申请

US20120034315A1 SOLID FORMS OF AN AZOCYCLIC AMIDE 有权
标题翻译： 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。

38. 发明授权

US08049029B2 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：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。

39. 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。

40. 发明申请

US20090156592A1 Fungicidal Azocyclic Amides 有权
标题翻译：杀真菌唑环酰胺
公开(公告)号：US20090156592A1
公开(公告)日：2009-06-18
申请号：US12303256
申请日：2007-07-27
申请人： Robert James Pasteris , Mary Ann Hanagan , Rafael Shapiro
发明人： Robert James Pasteris , Mary Ann Hanagan , Rafael Shapiro
IPC分类号： A01N43/80 , C07D417/14 , C07D231/12 , C07D231/16 , C07D401/14 , A01P3/00 , A01N43/78 , C07D413/00 , C07D413/14 , A01N43/84
CPC分类号： C07D495/10 , C07D211/62 , C07D263/14 , C07D401/06 , C07D401/14 , C07D413/04 , C07D417/04 , C07D417/14 , C07D498/10
摘要： Disclosed are compounds of Formulae 1, 1A, 1B and 1C including all geometric and stereoisomers, N-oxides, and salts thereof, wherein R1, R2, R4a1, R4a2, A, Aa, G, M, W, Z1, Z3, X, J, J1 and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
摘要翻译：公开了具有所有几何和立体异构体，N-氧化物及其盐的式1A，1B和1C的化合物，其中R1，R2，R4a1，R4a2，A，Aa，G，M，W，Z1，Z3，X ，J，J1和n如本公开中所定义。还公开了含有式1化合物的组合物和用于控制由真菌病原体引起的植物病害的方法，包括施用有效量的本发明化合物或组合物。

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