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1. 发明申请

WO2011131545A1 PROCESS FOR THE PREPARATION OF PYRAZOLE CARBOXYLIC ACID AMIDES 审中-公开
标题翻译：制备吡唑羧酸酰胺的方法
公开(公告)号：WO2011131545A1
公开(公告)日：2011-10-27
申请号：PCT/EP2011/055871
申请日：2011-04-14
申请人： SYNGENTA PARTICIPATIONS AG , DUMEUNIER, Raphael , SCHLETH, Florian , VETTIGER, Thomas , ROMMEL, Michael , TRAH, Stephan
发明人： DUMEUNIER, Raphael , SCHLETH, Florian , VETTIGER, Thomas , ROMMEL, Michael , TRAH, Stephan
IPC分类号： C07D231/14 , C07D303/17 , C07C35/52 , C07C25/24
CPC分类号： C07D231/14 , C07C17/23 , C07C17/30 , C07C25/24 , C07C29/132 , C07C35/52 , C07C45/29 , C07C209/10 , C07C2603/66 , C07D303/17 , C07C49/697 , C07C23/10 , C07C25/22 , C07C211/61
摘要： The invention relates to a process for the preparation of the compound of formula (I), which process comprises a) reacting a compound of formula (II), wherein X is chloro or bromo, with an organometallic species in an inert atmosphere to a halobenzyne of formula (X), reacting the halobenzyne of formula X so formed with cyclopentadiene to (III), b) reacting III in the presence of an inert solvent with an oxidant to (IV), c) reacing IV in the presence of a Lewis acid and a hydride source to (V), d) reacting V in the presence of an oxidizing agent, a base and an inert solvent to (VI), e) converting VI in the presence of a phosphane and CCl 4 or CHCl 3 to (VII), and either f1) reacting VII with NH 3 in the presence of a catalyst to the compound of formula (VIII); and g) reacting VIII in the presence of a base with a compound of formula (IX), to the compound of formula (I); or f2) reacting the compound of formula (VII), in the presence of a solvent, a base, a copper catalyst and at least one ligand with the compound of formula (IXa), to the compound of formula (I).
摘要翻译：本发明涉及一种制备式（I）化合物的方法，该方法包括：a）使惰性气氛中的有机金属物质使式（II）化合物（其中X为氯或溴）与卤代苯使式（X）所示的卤代苯与环戊二烯反应，（b）使惰性溶剂与惰性溶剂的存在下的III反应与式（Ⅳ）反应：c）在Lewis 酸和氢化物源至（V），d）使V在氧化剂，碱和惰性溶剂的存在下与（VI）反应，e）在磷烷和CCl 4或CHCl 3存在下将VI转化为（VII ），并且f1）使VII与NH 3在催化剂存在下与式（VIII）化合物反应; 和g）在碱存在下使VIII与式（IX）化合物反应，得到式（I）化合物; 或者f2）使式（Ⅶ）化合物在溶剂存在下，碱，铜催化剂和至少一种配体与式（Ⅸa）化合物反应，得到式（Ⅰ）化合物。

2. 发明申请

WO2011131544A1 PROCESS FOR THE PREPARATION OF PYRAZOLE CARBOXYLIC ACID AMIDES 审中-公开
标题翻译：制备吡唑羧酸酰胺的方法
公开(公告)号：WO2011131544A1
公开(公告)日：2011-10-27
申请号：PCT/EP2011/055870
申请日：2011-04-14
申请人： SYNGENTA PARTICIPATIONS AG , SCHLETH, Florian , VETTIGER, Thomas , ROMMEL, Michael , TOBLER, Hans
发明人： SCHLETH, Florian , VETTIGER, Thomas , ROMMEL, Michael , TOBLER, Hans
IPC分类号： C07D231/14 , C07C23/38
CPC分类号： C07D231/14 , C07C17/2635 , C07C17/30 , C07C17/354 , C07C25/24
摘要： The invention relates to a process for the preparation of a compound of formula (I), which process comprises a) reacting a compound of formula (II), wherein X is chloro or bromo, with an organometallic species to (III) reacting the halobenzyne of formula (III) so formed with (IV) wherein R 1 and R 2 are hydrogen or C 1 -C 6 alkyl; to (V), b) hydrogenating V in the presence of a metal catalyst to (VI), c) ozonising (VI) to (VII) d) converting (VII) in the presence of a phosphane and CCI 4 or CHCI 3 to (VIII) (VIII), and either e1 ) reacting VIII with NH 3 in the presence of a catalyst to (IX) and f) reacting IX in the presence of a base with the compound of formula (X), to the compound of formula (I); or e2) reacting the compound of formula (VIII), in the presence of a solvent, a base, a copper catalyst and at least one ligand with (Xa), to the compound of formula (I).
摘要翻译：本发明涉及一种制备式（I）化合物的方法，该方法包括：使式（II）化合物（其中X为氯或溴）与有机金属物质反应，使（III）使卤代苯甲（Ⅳ），其中R 1和R 2是氢或C 1 -C 6烷基; 至（V）中，b）在金属催化剂存在下将V氢化为（Ⅵ），c）臭氧化（Ⅵ）至（Ⅶ）d）在磷烷和CCI4或CHCl3存在下将（Ⅶ）转化为）（VIII），和e1）在催化剂存在下将VIII与NH 3反应至（IX），和f）使IX在碱的存在下与式（X）化合物反应至式（I ）; 或e2）使式（VIII）化合物在溶剂存在下，碱，铜催化剂和至少一种配体与（Xa）反应，得到式（I）化合物。

3. 发明申请

WO2011131546A1 PROCESS FOR THE PREPARATION OF PYRAZOLE CARBOXYLIC ACID AMIDES 审中-公开
标题翻译：制备吡唑羧酸酰胺的方法
公开(公告)号：WO2011131546A1
公开(公告)日：2011-10-27
申请号：PCT/EP2011/055872
申请日：2011-04-14
申请人： SYNGENTA PARTICIPATIONS AG , GRIBKOV, Denis , STOHLER, Remo , VETTIGER, Thomas , ROMMEL, Michael
发明人： GRIBKOV, Denis , STOHLER, Remo , VETTIGER, Thomas , ROMMEL, Michael
IPC分类号： C07D231/14 , C07C25/24
CPC分类号： C07D231/14 , C07C25/24
摘要： The invention relates to a process for the preparation of formula (I) which process comprises a) reacting a compound of formula (II), wherein X is chloro or bromo, with an organometallic species to (III), wherein X is chloro or bromo; reacting the halobenzyne with a fulvene (IV), to a compound of formula(V) wherein X is chloro or bromo; b) hydrogenating V in the presence of a suitable metal catalyst to a compound of formula (VI) wherein X is chloro or bromo; and either c1) reacting the compound of formula VI with NH3 in the presence of a catalyst comprising palladium and at least one ligand to the compound of formula (VII); and d) reacting the compound of formula VII in the presence of a base with a compound of formula (VIII), to the compound of formula I; or c2 reacting the compound of formula (VI) in the presence of a copper catalyst and a ligand with the compound of formula (VIIIa), to the compound of formula (I).
摘要翻译：本发明涉及一种制备式（I）的方法，该方法包括a）将其中X为氯或溴的式（II）化合物与有机金属物质反应为（III），其中X为氯或溴 ; 将卤代苯与富烯（Ⅳ）反应于其中X为氯或溴的式（Ⅴ）化合物; b）在合适的金属催化剂存在下将V氢化为其中X为氯或溴的式（Ⅵ）化合物; 并且c1）在包含钯和至少一种配体的催化剂存在下使式VI的化合物与NH 3反应到式（VII）的化合物; 和d）使式VII化合物在碱存在下与式（VIII）化合物反应，得到式I化合物; 或c2将式（VI）化合物在铜催化剂和配体的存在下与式（VIIIa）化合物反应，得到式（I）化合物。

4. 发明申请

WO2008031548A1 PROCESS FOR THE PREPARATION OF ANTHRANILAMIDE DERIVATIVES 审中-公开
标题翻译：制备蒽醌衍生物的方法
公开(公告)号：WO2008031548A1
公开(公告)日：2008-03-20
申请号：PCT/EP2007/007871
申请日：2007-09-10
申请人： SYNGENTA PARTICIPATIONS AG , VETTIGER, Thomas , STOLLER, André , JACKSON, David, Anthony
发明人： VETTIGER, Thomas , STOLLER, André , JACKSON, David, Anthony
IPC分类号： C07D401/04
CPC分类号： C07D401/04
摘要： The present invention relates to a process for the preparation of a compound of formula (I), by a) treating a compound of formula (Il), with a compound of formula (III), in the presence of a base to form a compound of formula (IV), and b) converting said compound of formula (IV) in the presence of an acid or base to the compound of formula (I).
摘要翻译：本发明涉及式（I）化合物的制备方法：a）在碱存在下，用式（III）化合物处理式（II）化合物，以形成化合物式（Ⅳ）化合物，和b）将式（Ⅳ）化合物在酸或碱的存在下转化成式（I）化合物。

5. 发明申请

WO2009007033A1 PROCESS FOR THE PRODUCTION OF AMINES 审中-公开
标题翻译：生产氨基酸的方法
公开(公告)号：WO2009007033A1
公开(公告)日：2009-01-15
申请号：PCT/EP2008/005338
申请日：2008-06-30
申请人： SYNGENTA PARTICIPATIONS AG , FUERST, Maren , VETTIGER, Thomas
发明人： FUERST, Maren , VETTIGER, Thomas
IPC分类号： C07C209/10 , C07C211/45
CPC分类号： C07C209/10 , C07C2601/02 , C07C211/45
摘要： The present invention relates to a process for the preparation of compounds of formula (I) wherein R 1 is C 6 -C 7 alkyl or a group (A 1 ) wherein R 2 , R 3 and R 4 are each independently of the others hydrogen or C 1 -C 4 alkyl; wherein a compound of formula (Il) wherein R 1 is as defined for formula (I) and X is bromine or chlorine, is reacted with urea in the presence of a base and a catalytic amount of at least one palladium complex compound, wherein the palladium complex compound comprises at least one ferrocenyl-biphosphine ligand.
摘要翻译：本发明涉及制备式（I）化合物的方法，其中R 1是C 6 -C 7烷基或其中R 2，R 3和R 4各自独立地是氢或C 1 -C 4烷基的基团（A1）其中R 1如式（I）所定义且X为溴或氯的式（II）化合物在碱和催化量的至少一种钯络合物存在下与脲反应，其中钯络合物包含至少一种二茂铁基 - 二膦配体。

6. 发明申请

WO2008145257A1 PROCESS FOR THE PRODUCTION OF PYRAZOLES 审中-公开
标题翻译：生产吡唑的方法
公开(公告)号：WO2008145257A1
公开(公告)日：2008-12-04
申请号：PCT/EP2008/003841
申请日：2008-05-13
申请人： SYNGENTA PARTICIPATIONS AG , GIORDANO, Fanny , VETTIGER, Thomas , WISS, Juerg, Gustav
发明人： GIORDANO, Fanny , VETTIGER, Thomas , WISS, Juerg, Gustav
IPC分类号： C07D231/14
CPC分类号： C07D231/14
摘要： A process for the production of a compound of formula (I), which comprises a) reacting a compound of formula (II), wherein R 1 and R 2 are both independently C 1 -C 6 alkyl, with methylhydrazine in the presence of water and a water-immiscible organic solvent being inert in saponification reactions, to form a compound of formula (III) wherein R 1 is as defined for formula (II) and b) saponifying that compound in sitυ leading to the formation of the compound of formula (I) by b1) adding a base to form the anion of the compound of formula (I) and then adding an; acid to form the compound of formula (I); or b2) adding an acid to form the compound of formula (I).
摘要翻译：一种制备式（I）化合物的方法，其包括：a）使式（II）化合物（其中R 1和R 2各自独立地为C 1 -C 6烷基）与甲基肼在水和水 - 不混溶的有机溶剂在皂化反应中是惰性的，以形成式（III）的化合物，其中R 1如式（II）所定义，b）在该位置上皂化该化合物。导致式（I）化合物的形成：b1）加入碱形成式（I）化合物的阴离子，然后加入; 酸形成式（I）化合物; 或b2）加入酸形成式（I）化合物。

7. 发明申请

WO2008031549A1 PROCESS FOR THE PREPARATION OF ANTHRANILAMIDE DERIVATIVES 审中-公开
标题翻译：制备蒽醌衍生物的方法
公开(公告)号：WO2008031549A1
公开(公告)日：2008-03-20
申请号：PCT/EP2007/007872
申请日：2007-09-10
申请人： SYNGENTA PARTICIPATIONS AG , VETTIGER, Thomas , STOLLER, André , JACKSON, David, Anthony
发明人： VETTIGER, Thomas , STOLLER, André , JACKSON, David, Anthony
IPC分类号： C07D401/04
CPC分类号： C07D401/04
摘要： The present invention relates to a process for the preparation of a compound of formula (I), wherein the substituents are defined as in claim 1, by a) reacting a compound of formula (V) with a compound of formula (Vl) wherein hal is halogen and R 1 is C 1 -C 6 alkyl in the presence of a base to a compound of formula (III); b) treating a compound of formula (Il) with said compound of formula (III) in the presence of a base to form a compound of formula (IV) and c) converting said compound of formula (IV) in the presence of an acid or a base to the compound of formula (I).
摘要翻译：本发明涉及制备式（I）化合物的方法，其中取代基如权利要求1所定义，通过a）使式（Ⅴ）化合物与式（Ⅵ）化合物反应，其中hal 是卤素，R 1是C 1 -C 6 -C 6烷基，在碱存在下与式（III）的化合物反应; b）在碱的存在下用式（III）化合物处理式（II）化合物以形成式（IV）化合物，和c）在酸存在下将所述式（Ⅳ）化合物或式（I）化合物的碱。

8. 发明申请

WO2007083090A3 PROCESS FOR THE PREPARATION OF URACIL DERIVATIVES 审中-公开
公开(公告)号：WO2007083090A3
公开(公告)日：2007-07-26
申请号：PCT/GB2007/000095
申请日：2007-01-15
申请人： SYNGENTA LIMITED , SYNGENTA PARTICIPATIONS AG , BEAUDEGNIES, Renaud , CASSAYRE, Jérôme , GOTT, Brian, David , JACKSON, David, Anthony , LÜTHY, Christoph , QUARANTA, Laura , VETTIGER, Thomas , WENGER, Jean , ZELLER, Martin
发明人： BEAUDEGNIES, Renaud , CASSAYRE, Jérôme , GOTT, Brian, David , JACKSON, David, Anthony , LÜTHY, Christoph , QUARANTA, Laura , VETTIGER, Thomas , WENGER, Jean , ZELLER, Martin
IPC分类号： C07D213/69 , C07C15/04
摘要： A process of making a compound of formula (I); the process comprising reacting a compound of formula (II); with a compound of formula (III) in which R 1 is Cl to C3 alkyl or Cl to C3 haloalkyl, R 2 is Cl to C3 alkyl, X 1 and X 2 are halogen R 3 is a C 1-6 alkanoic acid 1-6 alkyl ester residue R 4 is C 1-6 straight or branched-chain alkyl, such as methyl, ethyl, propyl or butyl, preferably ethyl.

9. 发明申请

WO2003042166A3 PROCESS FOR PREPARATION OF α-HYDROXYCARBOXYLIC ACID AMIDES 审中-公开
公开(公告)号：WO2003042166A3
公开(公告)日：2003-05-22
申请号：PCT/EP2002/012844
申请日：2002-11-15
申请人： SYNGENTA PARTICIPATIONS AG , ZELLER, Martin , FABER, Dominik , VETTIGER, Thomas , LAMBERTH, Clemens
发明人： ZELLER, Martin , FABER, Dominik , VETTIGER, Thomas , LAMBERTH, Clemens
IPC分类号： C07C231/02
摘要： The invention concerns a novel process for the preparation of 2-phenyl-2-hydroxy-N-[2-(3-alkoxy-4-hydroxyphenyl)-ethyl]-acetamides of the formula (I), wherein R 1 is alkyl, R 2 and R 3 are each independently hydrogen or alkyl, and R 4 is optionally substituted aryl or optionally substituted heteroaryl, which process comprises reacting a 2-(3-alkoxy-4-hydroxyphenyl)-ethylamine of the formula (II), wherein R 1 R 2 and R 3 are as defined above with a α-hydoxycarboxylic acid ester of the formula (III) or a dioxolanone of the formula (III)a, wherein R 4 is as defined above, and R 5 , R 6 and R 7 independently of each other are lower alkyl. The compounds of formula (I) are important intermediates for a novel group of fungicides derived from mandelic acid amides.

10. 发明申请

WO2003042166A2 PROCESS FOR PREPARATION OF $G(A)-HYDROXYCARBOXYLIC ACID AMIDES 审中-公开
标题翻译：制备DOLLAR G（A） - 羟基羧酸酰胺的方法
公开(公告)号：WO2003042166A2
公开(公告)日：2003-05-22
申请号：PCT/EP2002/012844
申请日：2002-11-15
申请人： SYNGENTA PARTICIPATIONS AG , ZELLER, Martin , FABER, Dominik , VETTIGER, Thomas , LAMBERTH, Clemens
发明人： ZELLER, Martin , FABER, Dominik , VETTIGER, Thomas , LAMBERTH, Clemens
IPC分类号： C07C233/00
CPC分类号： C07C233/22
摘要： The invention concerns a novel process for the preparation of 2-phenyl-2-hydroxy-N-[2-(3-alkoxy-4-hydroxyphenyl)-ethyl]-acetamides of the formula (I), wherein R 1 is alkyl, R 2 and R 3 are each independently hydrogen or alkyl, and R 4 is optionally substituted aryl or optionally substituted heteroaryl, which process comprises reacting a 2-(3-alkoxy-4-hydroxyphenyl)-ethylamine of the formula (II), wherein R 1 R 2 and R 3 are as defined above with a α-hydoxycarboxylic acid ester of the formula (III) or a dioxolanone of the formula (III)a, wherein R 4 is as defined above, and R 5 , R 6 and R 7 independently of each other are lower alkyl. The compounds of formula (I) are important intermediates for a novel group of fungicides derived from mandelic acid amides.
摘要翻译：本发明涉及制备式（I）的2-苯基-2-羟基-N- [2-（3-烷氧基-4-羟基苯基） - 乙基] - 乙酰胺的新方法，其中R1是烷基，R2 和R 3各自独立地为氢或烷基，且R 4为任选取代的芳基或任选取代的杂芳基，该方法包括使式（II）的2-（3-烷氧基-4-羟基苯基） - 乙基胺反应，其中R1R2和R3 如上所定义的式（III）的α-脱氧羧酸酯或式（III）a的二氧戊环酮，其中R 4如上所定义，R 5，R 6和R 7彼此独立地为低级烷基。式（I）化合物是衍生自扁桃酸酰胺的新型杀真菌剂组的重要中间体。

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