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1. 发明申请

WO2008013622A3 FUNGICIDAL AZOCYCLIC AMIDES 审中-公开
标题翻译：杀菌剂AZOCYCLIC酰胺
公开(公告)号：WO2008013622A3
公开(公告)日：2008-03-27
申请号：PCT/US2007014647
申请日：2007-06-22
申请人： DU PONT , PASTERIS ROBERT JAMES , HANAGAN MARY ANN , SHAPIRO RAFAEL
发明人： PASTERIS ROBERT JAMES , HANAGAN MARY ANN , SHAPIRO RAFAEL
IPC分类号： A61K31/454
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, insert Formulae 1, 1A, 1B and 1C here wherein R 1 , R 2 , R 4a1 , R 4a2 , A, A a , G, M, W, Z 1 , Z 3 , X, J, J 1 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：公开了式1,1A，1B和1C的化合物，其包括所有的几何和立体异构体，N氧化物及其盐，插入式1,1A，1B和1C，其中R 1，R 1， 2，R 4a1，R 4a2，A，A a，G，M，W，Z 1， Z，X，J，J 1和n如本发明中所定义。还公开了含有式1化合物的组合物和用于防治由真菌病原体引起的植物病害的方法，所述方法包括施用有效量的本发明化合物或组合物。

2. 发明申请

WO2008013925A4 FUNGICIDAL AZOCYCLIC AMIDES 审中-公开
标题翻译：杀真菌剂
公开(公告)号：WO2008013925A4
公开(公告)日：2010-09-30
申请号：PCT/US2007016875
申请日：2007-07-27
申请人： DU PONT , PASTERIS ROBERT JAMES , HANAGAN MARY ANN , SHAPIRO RAFAEL
发明人： PASTERIS ROBERT JAMES , HANAGAN MARY ANN , SHAPIRO RAFAEL
IPC分类号： A61K31/454
CPC分类号： C07D417/14 , A01N43/56 , C07D403/14 , C07D413/14 , 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。

3. 发明申请

WO2008013925A3 FUNGICIDAL AZOCYCLIC AMIDES 审中-公开
标题翻译：杀菌剂AZOCYCLIC酰胺
公开(公告)号：WO2008013925A3
公开(公告)日：2008-04-03
申请号：PCT/US2007016875
申请日：2007-07-27
申请人： DU PONT , PASTERIS ROBERT JAMES , HANAGAN MARY ANN , SHAPIRO RAFAEL
发明人： PASTERIS ROBERT JAMES , HANAGAN MARY ANN , SHAPIRO RAFAEL
IPC分类号： A61K31/454
CPC分类号： C07D417/14 , A01N43/56 , C07D403/14 , C07D413/14 , 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 R 1 , R 2 , R 4a1 , R4 a2 , A, A a , G, M, W, Z 1 , Z 3 , X, J, J 1 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：公开了式1,1A，1B和1C的化合物，包括所有几何和立体异构体，N-氧化物和盐，其中R 1，R 2，R 3，R 3， > 4a1，R4a2，A，Aa，G，M，W，Z1，Z3， X，J，J 1和n如本发明中所定义。还公开了含有式1化合物的组合物和用于防治由真菌病原体引起的植物病害的方法，所述方法包括施用有效量的本发明化合物或组合物。

4. 发明申请

WO2006121648A3 METHOD FOR PREPARATION OF OPTIONALLY 2-SUBSTITUTED 1,6-DIHYDRO-6-OXO-4-PYRIMIDINECARBOXYLIC ACIDS 审中-公开
标题翻译：选择性取代的2-取代的1,6-二羟基-6-氧代-4-吡啶羧酸的方法
公开(公告)号：WO2006121648A3
公开(公告)日：2006-12-28
申请号：PCT/US2006016340
申请日：2006-04-28
申请人： DU PONT , SHAPIRO RAFAEL
发明人： SHAPIRO RAFAEL
IPC分类号： C07D239/28 , A61K31/505
CPC分类号： C07D239/28
摘要： A new method for the preparation of optionally 2-substituted 1,6-dihydro-6-oxo-4 pyrimidinecarboxylic acid compounds of formula (1) is disclosed wherein R 1 is H or an optionally substituted carbon moiety. Also disclosed is the method comprising additional steps to prepare optionally substituted 4 pyrimidine-carboxylic acids and esters using the compound of formula (1) as an intermediate.
摘要翻译：公开了用于制备式（1）的任选的2-取代的1,6-二氢-6-氧代-4嘧啶羧酸化合物的新方法，其中R 1是H或任选取代的碳部分。还公开了包括使用式（1）化合物作为中间体制备任选取代的4嘧啶羧酸和酯的附加步骤的方法。

5. 发明申请

WO2008010897A3 PROCESS FOR MAKING 3-SUBSTITUTED 2-AMINO-5-HALOBENZAMIDES 审中-公开
标题翻译：制备3-取代的2-氨基-5-羟基苯甲酸的方法
公开(公告)号：WO2008010897A3
公开(公告)日：2009-05-07
申请号：PCT/US2007014972
申请日：2007-06-27
申请人： DU PONT , DAVIS RICHARD FRANK , SHAPIRO RAFAEL , TAYLOR ERIC DEGUYON
发明人： DAVIS RICHARD FRANK , SHAPIRO RAFAEL , TAYLOR ERIC DEGUYON
IPC分类号： C07C231/02 , C07C237/30 , C07C271/28 , C07D265/14 , C07D401/04
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. ( 1, 2, 4 ) wherein R1 is H, C1_C4 alkyl, cyclopropyl, cyclopropylmethyl or methylcyclopropyl; R2 is CH3 or C1; R3 is C1_C6alkyl or C3_ C6 alkenyl, each optionally substituted with up to 3 halogen and up to 1 phenyl; and X is C1 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。（1,2,4）其中R 1是H，C 1 -C 4烷基，环丙基，环丙基甲基或甲基环丙基; R2是CH3或C1; 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C1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，使用通过上述方法制备式1化合物的式1化合物。

6. 发明申请

WO2008082502A3 PROCESS FOR PREPARING 2-AMINO-5-CYANOBENZOIC ACID DERIVATIVES 审中-公开
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：WO2008082502A3
公开(公告)日：2008-10-16
申请号：PCT/US2007025800
申请日：2007-12-18
申请人： DU PONT , ANNIS GARY DAVID , BRUENING JOERG , CURRIE MARTIN JAMES , DUMAS DONALD JOSEPH , SHAPIRO RAFAEL
发明人： ANNIS GARY DAVID , BRUENING JOERG , CURRIE MARTIN JAMES , DUMAS DONALD JOSEPH , SHAPIRO RAFAEL
IPC分类号： C07C231/12 , C07C233/65 , C07C253/14 , C07C255/58 , C07D401/04
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 R 1 is NHR 3 or OR 4 ; R 2 is CH 3 or Cl; R 3 is H, C 1 -C 4 alkyl, cyclopropyl, cyclopropylcyclopropyl, cyclopropylmethyl or methylcyclopropyl; R 4 is H or C 1 -C 4 alkyl; Y is Br or Cl; X is NR 13 or O; n is 0 or 1; and R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 11 , R 12 and R 13 are as defined in the disclosure. Also disclosed is a method for preparing a compound of Formula (2) wherein Y is Br and R 1 is NHR 3 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 R 14 , R 15 , R 16 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：公开了用于制备式（1）化合物的方法，其包括使式（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）化合物接触，：其中R SUB1是NHR SUB3或OR SUB4。 R _{2 是CH _{3 或CI; R 3是H，C 1 -C 4烷基，环丙基，环丙基环丙基，环丙基甲基或甲基环丙基; R 4是H或C 1 -C 4烷基; Y是Br或Cl; X是NR 13或O; n是0或1; 和R SUB 5，R SUB 6，R SUB 7，R SUB 8，R SUB 9，SUB 9，，R 10，R 11，R 12，R 13和R 13如本发明中所定义。还公开了制备式（2）化合物的方法，其中Y是Br并且R 1是NHR 3，包括将含溴气体引入含有化合物（4）所示的化合物，并进一步公开了用于制备其中R 14，R 15，R 16，SUB，和Z如本公开中所定义，使用式（1）化合物，其特征在于通过上述公开的方法制备式（1）化合物。}}

7. 发明申请

WO2005070888A3 PROCESS FOR THE MANUFACTURE OF 2,3-DICHLOROPYRIDINE 审中-公开
标题翻译：制备2,3-二氯吡啶的方法
公开(公告)号：WO2005070888A3
公开(公告)日：2005-10-20
申请号：PCT/US2005002462
申请日：2005-01-21
申请人： DU PONT , SHAPIRO RAFAEL
发明人： SHAPIRO RAFAEL
IPC分类号： C07D213/61 , C07D213/73 , C07D213/82
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存在下接触以形成重氮盐; 并且重氮盐随后在铜催化剂存在下分解，其中至少约50％的铜是铜（II）氧化态。

8. 发明申请

WO2007001385B1 PROCESS FOR PREPARING 4,5-DIHYDRO-PYRAZOLO [3,4-C] PYRID-2-ONES 审中-公开
标题翻译：制备4,5-二氢吡唑并[3,4-C]吡啶-2-酮的方法
公开(公告)号：WO2007001385B1
公开(公告)日：2007-07-12
申请号：PCT/US2005034548
申请日：2005-09-27
申请人： SQUIBB BRISTOL MYERS CO , SHAPIRO RAFAEL , ROSSANO LUCIUS T , MUDRYK BOGUSLAW M , CUNIERE NICOLAS , OBERHOLZER MATTHEW , ZHANG HUIPING , CHEN BANG-CHI
发明人： SHAPIRO RAFAEL , ROSSANO LUCIUS T , MUDRYK BOGUSLAW M , CUNIERE NICOLAS , OBERHOLZER MATTHEW , ZHANG HUIPING , CHEN BANG-CHI
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： A novel process and intermediates thereof for making 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones of the type shown below from appropriate phenyl hydrazines is described. These compounds can be useful as factor Xa inhibitors.
摘要翻译：描述了从合适的苯基肼制备下文所示类型的4,5-二氢 - 吡唑并[3,4-c]吡啶-2-酮的新方法和中间体。这些化合物可用作Xa因子抑制剂。

9. 发明申请

WO2006036498A3 A PROCESS FOR THE PREPARATION OF 1,3,5-TRISUBSTITUTED PYRAZOLES VIA [3+2] CYCLOADDITION 审中-公开
标题翻译：通过[3 + 2]环加成制备1,3,5-三唑基吡咯的方法
公开(公告)号：WO2006036498A3
公开(公告)日：2007-07-12
申请号：PCT/US2005032050
申请日：2005-09-07
申请人： SQUIBB BRISTOL MYERS CO , ROSSANO LUCIUS T , SHAPIRO RAFAEL , TENHUISEN KAREN L
发明人： ROSSANO LUCIUS T , SHAPIRO RAFAEL , TENHUISEN KAREN L
IPC分类号： C07D231/10
CPC分类号： C07D231/14
摘要： A process for the preparation of 1,3,5-trisubstituted pyrazole compounds, which are useful intermediates in the synthesis of factor Xa inhibitors.
摘要翻译：制备1,3,5-三取代吡唑化合物的方法，其在合成因子Xa抑制剂中是有用的中间体。

10. 发明申请

WO2007001385A3 PROCESS FOR PREPARING 4,5-DIHYDRO-PYRAZOLO [3,4-C] PYRID-2-ONES 审中-公开
标题翻译：制备4,5-二羟基 - 吡唑并[3,4-C]吡啶-2-酮的方法
公开(公告)号：WO2007001385A3
公开(公告)日：2007-05-31
申请号：PCT/US2005034548
申请日：2005-09-27
申请人： SQUIBB BRISTOL MYERS CO , SHAPIRO RAFAEL , ROSSANO LUCIUS T , MUDRYK BOGUSLAW M , CUNIERE NICOLAS , OBERHOLZER MATTHEW , ZHANG HUIPING , CHEN BANG-CHI
发明人： SHAPIRO RAFAEL , ROSSANO LUCIUS T , MUDRYK BOGUSLAW M , CUNIERE NICOLAS , OBERHOLZER MATTHEW , ZHANG HUIPING , CHEN BANG-CHI
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： A novel process and intermediates thereof for making 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones of the type shown below from appropriate phenyl hydrazines is described. These compounds can be useful as factor Xa inhibitors.
摘要翻译：描述了由合适的苯肼制备下列所示类型的4,5-二氢 - 吡唑并[3,4-c]吡啶-2-酮的新方法及其中间体。这些化合物可用作因子Xa抑制剂。

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