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1. 发明授权

US07009058B1 Method for preparing pyridine-2,3-dicarboxylic acid esters 失效
标题翻译：制备吡啶-2,3-二羧酸酯的方法
公开(公告)号：US07009058B1
公开(公告)日：2006-03-07
申请号：US09568993
申请日：2000-05-11
申请人： Yves Bessard , Gerhard Stucky , Jean-Paul Roduit
发明人： Yves Bessard , Gerhard Stucky , Jean-Paul Roduit
IPC分类号： C07D213/80 , C07D213/803
CPC分类号： C07D213/803 , C07D213/61 , C07D213/80
摘要： A method for preparing pyridine-2,3-dicarboxylic acid esters of the general formula: wherein R is C1-6-alkyl, C3-6-cycloalkyl, aryl or arylalkyl, and R1 to R3, independently of one another, represent hydrogen, C1-6-alkyl, fluorinated C1-6-alkyl, C1-6-alkoxy, (C1-6-alkoxy)-C1-6-alkyl or (C1-6-alkoxy)carbonyl. These esters are obtained from the corresponding 2,3-dichloropyridine, the corresponding alcohol ROH and carbon monoxide in the presence of a palladium-diphosphine complex and a weak base. Pyridine-2,3-dicarboxylic acid esters are herbicides or intermediates for the preparation of herbicides.
摘要翻译：制备以下通式的吡啶-2,3-二羧酸酯的方法：其中R是C 1-6 - 烷基，C 3-6 - 环烷基，芳基或芳基烷基，R 1至R 3彼此独立地表示氢，C 1-6 - 烷基，氟化C

2. 发明授权

US5821368A Method for preparing pyrimidin-2-ylacetic acid esters 失效
标题翻译：制备嘧啶-2-基乙酸酯的方法
公开(公告)号：US5821368A
公开(公告)日：1998-10-13
申请号：US889442
申请日：1997-07-08
申请人： Yves Bessard , Gerhard Stucky
发明人： Yves Bessard , Gerhard Stucky
IPC分类号： B01J31/24 , C07B61/00 , C07D239/52 , C07D239/34 , C07D239/26
CPC分类号： C07D239/52
摘要： A method for preparing pyrimidin-2-ylacetic acid esters of the general formula: ##STR1## wherein R is C.sub.1-6 -alkyl, C.sub.3-6 -cycloalkyl, aryl or arylalkyl and R.sup.1 to R.sup.3, independently of one another, are hydrogen, C.sub.1-6 -alkyl, fluorinated C.sub.1-6 -alkyl, C.sub.1-6 -alkoxy, (C.sub.1-6 -alkoxy)-C.sub.1-6 -alkyl or (C.sub.1-6 -alkoxy)carbonyl. These esters are obtained from the corresponding 2-(halomethyl)-pyrimidine, the corresponding alcohol ROH and carbon monoxide in the presence of a palladium-phosphine complex and a base. Pyrimidin-2-ylacetic acid esters are intermediates in the preparation of herbicides.
摘要翻译：制备通式如下的嘧啶-2-基乙酸酯的方法：其中R是C 1-6 - 烷基，C 3-6 - 环烷基，芳基或芳基烷基和R 1 -R 3，彼此独立地是氢，C 1-6 - 烷基，氟化C 1-6 - 烷基，C 1-6 - 烷氧基，（C 1-6 - 烷氧基）-C 1-6 - 烷基或（C 1-6 - 烷氧基）羰基。这些酯在钯 - 膦配合物和碱的存在下由相应的2-（卤代甲基） - 嘧啶，相应的醇ROH和一氧化碳获得。嘧啶-2-基乙酸酯是制备除草剂的中间体。

3. 发明授权

US5583226A 4,6-dichloropyrimidine and related compounds 失效
标题翻译： 4,6-二氯嘧啶和相关化合物
公开(公告)号：US5583226A
公开(公告)日：1996-12-10
申请号：US428916
申请日：1995-04-25
申请人： Gerhard Stucky , Rene Imwinkelried
发明人： Gerhard Stucky , Rene Imwinkelried
IPC分类号： A61K31/70 , A61P31/12 , C07D239/48
CPC分类号： C07D239/48
摘要： A novel pyrimidine derivative, N-(2-amino-4,6-dichloropyrimidine-5-yl)formamide for use, e.g., in the production of antiviral nucleotide derivatives, can be made by a process involving cyclyzing an aminomalonic ester with guanidine or its salt in the presence of a base to produce 2,5-diamino-4,6-dihydroxypyrimidine or its salt, chlorinating this product with a chlorinating agent in the presence of an amide to produce 4,6-dichloropyrimidine, and reacting the 4,6-dichlororpyrimidine with an aqueous solution of a carboxylic acid to produce the N-(2-amino-4,6-dichloropyrimidine-5-yl)formammide. Novel also are 4,6-dichloropyrimidine, 4,6-dichloro-N'-(dimethylaminomethylene)pyrimidine-2,5-diamine, 4,6-dichloro-N'-(piperidine-1-ylmethylene)pyrimidine-2,5-diamine, and a process for making 2,5-diamino-4,6-dichloropyrimidine.
摘要翻译：用于制备抗病毒核苷酸衍生物的新颖的嘧啶衍生物N-（2-氨基-4,6-二氯嘧啶-5-基）甲酰胺可以通过一种方法制备，该方法包括用胍或氨基马来酸酯其盐在碱的存在下反应以产生2,5-二氨基-4,6-二羟基嘧啶或其盐，在酰胺存在下用氯化剂氯化该产物以产生4,6-二氯嘧啶，并使4 ，6-二氯 - 嘧啶与羧酸的水溶液反应，得到N-（2-氨基-4,6-二氯嘧啶-5-基）甲酰胺。新颖的还有4,6-二氯嘧啶，4,6-二氯-N' - （二甲基氨基亚甲基）嘧啶-2,5-二胺，4,6-二氯-N' - （哌啶-1-基亚甲基）嘧啶-2,5 - 二胺，以及制备2,5-二氨基-4,6-二氯嘧啶的方法。

4. 发明授权

US6114527A Process for preparing substituted pyrimidine derivatives 失效
标题翻译：制备取代嘧啶衍生物的方法
公开(公告)号：US6114527A
公开(公告)日：2000-09-05
申请号：US341540
申请日：1999-12-17
申请人： Beat Schmidt , Gerhard Stucky
发明人： Beat Schmidt , Gerhard Stucky
IPC分类号： C07D239/36 , C07D239/40 , C07D239/02
CPC分类号： C07D239/36 , C07D239/40
摘要： A process for preparing substituted pyrimidine derivatives of the general formula (I): in which a [3-(dimethylamino)-2-azaprop-2-en-1-ylidine]dimethylammonium halide is reacted with a substituted acetamide. The compounds of general formula (I) are important intermediate products for pharmaceutical or agrochemical active substances.
摘要翻译： PCT No.PCT / EP98 / 00074 Sec。 371 1999年12月17日第 102（e）1999年12月17日PCT PCT 1998年1月8日PCT公布。第WO98 / 30549号公报日期1998年7月16日制备通式（I）的取代嘧啶衍生物的方法：其中[3-（二甲基氨基）-2-氮杂丙-2-烯-1-基]二甲基卤化铵与取代的乙酰胺。通式（I）的化合物是药物或农药活性物质的重要中间产物。

5. 发明授权

US5663340A N-(2-amino-4,6-dichloropyrimidine-5-yl)formamide, and a process for its preparation 失效
标题翻译： N-（2-氨基-4,6-二氯嘧啶-5-基）甲酰胺及其制备方法
公开(公告)号：US5663340A
公开(公告)日：1997-09-02
申请号：US693520
申请日：1996-08-08
申请人： Gerhard Stucky , Rene Imwinkelried
发明人： Gerhard Stucky , Rene Imwinkelried
IPC分类号： A61K31/70 , A61P31/12 , C07D239/48
CPC分类号： C07D239/48
摘要： A novel pyrimidine derivative, N-(2-amino-4,6-dichloropyrimidine-5-yl) formamide for use, e.g., in the production of antiviral nucleotide derivatives, can be made by a process involving cyclyzing an aminomalonic ester with guanidine or its salt in the presence of a base to produce 2,5-diamino-4,6-dihydroxypyrimidine or its salt, chlorinating this product with a chlorinating agent in the presence of an amide to produce 4,6-dichloropyrimidine, and reacting the 4,6-dichlororpyrimidine with an aqueous solution of a carboxylic acid to produce the N-(2-amino-4,6-dichloropyrimidine-5-yl) formamide. Novel also are 4,6-dichloropyrimidine, 4,6-dichloro-N'-(dimethylamino-methylene) pyrimidine-2,5-diamine, 4,6-dichloro-N'-(piperidine-1-ylmethylene) pyrimidine-2,5-diamine, and a process for making 2,5-diamino-4,6-dichloropyrimidine.
摘要翻译：用于制备抗病毒核苷酸衍生物的新颖的嘧啶衍生物N-（2-氨基-4,6-二氯嘧啶-5-基）甲酰胺可以通过一种方法制备，该方法包括用胍或氨基马来酸酯其盐在碱的存在下反应以产生2,5-二氨基-4,6-二羟基嘧啶或其盐，在酰胺存在下用氯化剂氯化该产物以产生4,6-二氯嘧啶，并使4 ，6-二氯 - 嘧啶与羧酸的水溶液反应，得到N-（2-氨基-4,6-二氯嘧啶-5-基）甲酰胺。新颖的还有4,6-二氯嘧啶，4,6-二氯-N' - （二甲基氨基 - 亚甲基）嘧啶-2,5-二胺，4,6-二氯-N' - （哌啶-1-基亚甲基）嘧啶-2 ，5-二胺，以及制备2,5-二氨基-4,6-二氯嘧啶的方法。

6. 发明授权

US5591853A Products of a microbiological process for the production of 2-halo-pyrimidine-4-carboxylic acids 失效
标题翻译：用于生产2-卤代嘧啶-4-羧酸的微生物过程的产物
公开(公告)号：US5591853A
公开(公告)日：1997-01-07
申请号：US344122
申请日：1994-11-23
申请人： Andreas Kiener , Rainer Gl ockler , Gerhard Stucky
发明人： Andreas Kiener , Rainer Gl ockler , Gerhard Stucky
IPC分类号： C12P7/02 , C07D239/08 , C07D239/30 , C12P9/00 , C12P17/00 , C12P17/12 , C12R1/40 , C07D239/26 , C07D239/34
CPC分类号： C07D239/30 , C12P17/12 , C12R1/40
摘要： A 2-halo-pyrimidine-4-carboxylic acid of formula: ##STR1## wherein X is a halogen atom, for example, 2-chloro-pyrimidine-4-carboxylic acid. A 2-substituted-pyrimidine-4-carboxylic acid derivative of formula: ##STR2## wherein R.sub.1 is a halogen atom, NH.sub.2 --, HO-- or a C.sub.1 -C.sub.4 alkoxy group and R.sub.2 is a C.sub.1 -C.sub.4 alkoxy group or a halogen atom with the proviso that, if R.sub.1 is a HO-- group, R.sub.2 is not a halogen atom and with the proviso that, if R.sub.2 is a halo group, R.sub.1 is not an amino group. A 2-substituted-pyrimidine-4-carboxylic acid derivative of formula III wherein R.sub.1 is a HO-- group and R.sub.2 is an ethoxy group.
摘要翻译：具有下式的其中X是卤素原子的2-卤代 - 嘧啶-4-羧酸，例如2-氯 - 嘧啶-4-甲酸。 2-取代的嘧啶-4-羧酸衍生物，其结构式如下：其中R1是卤素原子，NH2-，HO-或C1-C4烷氧基，R2是C1-C4烷氧基或卤素原子，条件是，如果R1是HO-基团，则R2不是卤素原子，条件是如果R2是卤素基团，则R1不是氨基。式III的2-取代 - 嘧啶-4-羧酸衍生物，其中R1是HO-基团，R2是乙氧基。

7. 发明授权

US5294710A N-5-protected 2,5-diamino-4,6-dichloropyrimidines and process for their production 失效
标题翻译： N-5保护的2,5-二氨基-4,6-二氯嘧啶及其生产方法
公开(公告)号：US5294710A
公开(公告)日：1994-03-15
申请号：US6525
申请日：1993-01-21
申请人： Gerhard Stucky , Felix Previdoli
发明人： Gerhard Stucky , Felix Previdoli
IPC分类号： C07D239/48 , C07D20060101 , C07D239/54 , C07D239/545 , C07D239/42 , C07D239/30 , C07D239/52
CPC分类号： C07D239/48 , C07D239/545
摘要： N-5-protected 2,5-diamino-4,6-dichloropyrimidines of general formula: ##STR1## wherein R is an alkoxy group or a trifluorometyl group, are valuable intermediate products for the production of pharmaceutical agents with antiviral properties. The above-mentioned compounds are produced by cyclization of an N protected amino malonic acid ester with guanidine in the presence of an alkali alcoholate and then chlorination of the resulting N-5-protected 4,6-dihydroxy-2,5-diaminopyrimidine.
摘要翻译：具有通式为：其中R是烷氧基或三氟甲基的通式为N-5保护的2,5-二氨基-4,6-二氯嘧啶是制备具有抗病毒性质的药剂的有价值的中间产物。上述化合物是通过在碱性醇化物的存在下使N保护的氨基丙二酸酯与胍进行环化而制得的，然后氯化得到的N-5-保护的4,6-二羟基-2,5-二氨基嘧啶。

8. 发明授权

US6162921A Process for preparing pyridinecarboxylic esters 失效
标题翻译：制备吡啶羧酸酯的方法
公开(公告)号：US6162921A
公开(公告)日：2000-12-19
申请号：US399744
申请日：1999-09-20
申请人： Yves Bessard , Gerhard Stucky , Jean-Paul Roduit
发明人： Yves Bessard , Gerhard Stucky , Jean-Paul Roduit
IPC分类号： C07D213/803 , B01J31/24 , C07B61/00 , C07D213/61 , C07D213/79 , C07D213/80 , C07D213/30
CPC分类号： C07D213/79 , C07D213/61 , C07D213/80
摘要： A process for preparing pyridinecarboxylic esters of the general formula: ##STR1## wherein R.sup.1 is hydrogen, a C.sub.1 -C.sub.6 -alkyl group, a C.sub.1 -C.sub.4 -alkoxycarbonyl group or a C.sub.1 -C.sub.4 -alkoxymethyl group, R.sup.2 is a C.sub.1 -C.sub.4 -alkyl group and X is chlorine or bromine. The pyridinecarboxylic esters are obtained by reacting the corresponding 2,3-dihalopyridines with carbon monoxide and a C.sub.1 -C.sub.4 -alkanol in the presence of a weak base and a complex of palladium with a bis(diphenylphosphine). Pyridinecarboxylic esters are intermediates for preparing herbicides and drugs against fibrotic diseases.
摘要翻译：一种制备通式如下的吡啶羧酸酯的方法：其中R 1是氢，C 1 -C 6烷基，C 1 -C 4烷氧基羰基或C 1 -C 4烷氧基甲基，R 2是C 1 -C 4烷基和 X是氯或溴。吡啶羧酸酯通过在弱碱和钯与双（二苯基膦）的络合物存在下，使相应的2,3-二卤代吡啶与一氧化碳和C 1 -C 4烷醇反应而获得。吡啶羧酸酯是制备除草剂和抗纤维化疾病药物的中间体。

9. 发明授权

US5925765A Process for preparing pyridinecarboxylic esters 失效
公开(公告)号：US5925765A
公开(公告)日：1999-07-20
申请号：US893152
申请日：1997-07-15
申请人： Yves Bessard , Gerhard Stucky , Jean-Paul Roduit
发明人： Yves Bessard , Gerhard Stucky , Jean-Paul Roduit
IPC分类号： C07D213/803 , B01J31/24 , C07B61/00 , C07D213/61 , C07D213/79 , C07D213/80 , C07D213/30
CPC分类号： C07D213/79 , C07D213/61 , C07D213/80
摘要： A process for preparing pyridinecarboxylic esters of the general formula: ##STR1## wherein R.sup.1 is hydrogen, a C.sub.1 -C.sub.6 -alkyl group, a C.sub.1 -C.sub.4 -alkoxycarbonyl group or a C.sub.1 -C.sub.4 -alkoxymethyl group, R.sup.2 is a C.sub.1 -C.sub.4 -alkyl group and X is chlorine or bromine. The pyridinecarboxylic esters are obtained by reacting the corresponding 2,3-dihalopyridines with carbon monoxide and a C.sub.1 -C.sub.4 -alkanol in the presence of a weak base and a complex of palladium with a bis(diphenylphosphine). Pyridinecarboxylic esters are intermediates for preparing herbicides and drugs against fibrotic diseases.

10. 发明授权

US5840892A Process for the preparation of substituted pyrimidines 失效
标题翻译：制备取代嘧啶的方法
公开(公告)号：US5840892A
公开(公告)日：1998-11-24
申请号：US838321
申请日：1997-04-08
申请人： Yves Bessard , Gerhard Stucky
发明人： Yves Bessard , Gerhard Stucky
IPC分类号： B01J31/02 , C07B61/00 , C07D239/34 , C07D239/46 , C07D239/52 , C07D239/56 , C07D239/60 , C07D401/12 , C07D405/04 , C07D405/12 , C07D407/12 , C07D401/06
CPC分类号： C07D239/60 , C07D239/34 , C07D405/04
摘要： A novel process for the preparation of substituted pyrimidine derivatives of the general formula: ##STR1## in which a halopyrimidine is reacted in the presence of a sulfinate with a compound selected from the series: ##STR2## The compounds of the general formula I are precursors of, for example, compounds with herbicidal activity.
摘要翻译：一种用于制备通式如下的取代嘧啶衍生物的新方法：在亚磺酸盐存在下与选自下列化合物的化合物：IIIc化合物通式Ⅰ化合物是前体例如具有除草活性的化合物。

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