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    • 1. 发明授权
    • N-(2-amino-4,6-dichloropyrimidine-5-yl)formamide, and a process for its
preparation
    • N-(2-氨基-4,6-二氯嘧啶-5-基)甲酰胺及其制备方法
    • US5663340A
    • 1997-09-02
    • US693520
    • 1996-08-08
    • Gerhard StuckyRene Imwinkelried
    • Gerhard StuckyRene Imwinkelried
    • A61K31/70A61P31/12C07D239/48
    • C07D239/48
    • 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.
    • 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。
    • 2. 发明授权
    • N-(2-amino-4,6-dichloropyrimidine-5-yl) formamide and a process for its
preparation
    • N-(2-氨基-4,6-二氯嘧啶-5-基)甲酰胺及其制备方法
    • US5693800A
    • 1997-12-02
    • US693521
    • 1996-08-08
    • Gerhard StuckyRene Imwinkelried
    • Gerhard StuckyRene Imwinkelried
    • A61K31/70A61P31/12C07D239/48
    • C07D239/48
    • 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-dichloropyrimidine 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'-(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 of the formula ##STR1##
    • 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,以及制备式(IMAGE)的2,5-二氨基-4,6-二氯嘧啶的方法
    • 3. 发明授权
    • Process for preparing imidazopyridine derivatives
    • 制备咪唑并吡啶衍生物的方法
    • US5446160A
    • 1995-08-29
    • US308448
    • 1994-09-19
    • Gerhard StuckyRene Imwinkelried
    • Gerhard StuckyRene Imwinkelried
    • C07D471/04C07D519/00
    • C07D471/04
    • A new process for preparing imidazopyridines of the general formula: ##STR1## wherein R.sub.1 is an alkyl, cycloalkyl, aryl or aralkyl group or is a heterocyclic radical, R.sub.2 and R.sub.4 are identical or different and are hydrogen, a hydroxy, a cyano, alkyl, cycloalkyl, aryl or aralkyl group or are an alkanoyl or an alkoxy-carbonyl group, and R.sub.3 is hydrogen, an alkyl, aryl or aralkyl group or a halogen atom. In the key step of the process, an imidate of the formula: ##STR2## is cyclized with aminoacetonitrile and a 1,3-dicarbonyl compound of the general formula: ##STR3## The imidazopyridines are valuable intermediates for the preparation of angiotensin II antagonists.
    • 一种制备通式如下的咪唑并吡啶的新方法:其中R 1是烷基,环烷基,芳基或芳烷基或是杂环基,R 2和R 4相同或不同,是氢,羟基,氰基, 烷基,环烷基,芳基或芳烷基,或者是烷酰基或烷氧基 - 羰基,R3是氢,烷基,芳基或芳烷基或卤素原子。 在该方法的关键步骤中,具有以下通式的亚胺基化合物:使用氨基乙腈和具有以下通式的1,3-二羰基化合物: III环化。 咪唑并吡啶是制备血管紧张素II拮抗剂的有价值的中间体。
    • 5. 发明授权
    • N-(2-amino-4, 6-dichlopyrimidine-5-yl) formanide, and a process for its
preparation
    • N-(2-氨基-4,6-二氯嘧啶-5-基)甲酰胺及其制备方法
    • US5744601A
    • 1998-04-28
    • US854378
    • 1997-05-12
    • Gerhard StuckyRene Imwinkelried
    • Gerhard StuckyRene Imwinkelried
    • A61K31/70A61P31/12C07D239/48
    • C07D239/48
    • 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'-(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.
    • 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
    • 4,6-dichloropyrimidine and related compounds
    • 4,6-二氯嘧啶和相关化合物
    • US5583226A
    • 1996-12-10
    • US428916
    • 1995-04-25
    • Gerhard StuckyRene Imwinkelried
    • Gerhard StuckyRene Imwinkelried
    • A61K31/70A61P31/12C07D239/48
    • C07D239/48
    • 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.
    • 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。