公开(公告)号：US5869683A

公开(公告)日：1999-02-09

申请号：US962648

申请日：1997-11-03

申请人： Hisayoshi Jonishi ,  Tokiya Kimura ,  Fumio Kanamori ,  Shigehisa Kanbayashi ,  Tooru Wakabayashi ,  Fumihiro Fukui ,  Akimasa Takenaka ,  Noriyuki Horiuchi

发明人： Hisayoshi Jonishi ,  Tokiya Kimura ,  Fumio Kanamori ,  Shigehisa Kanbayashi ,  Tooru Wakabayashi ,  Fumihiro Fukui ,  Akimasa Takenaka ,  Noriyuki Horiuchi

IPC分类号： C07C45/63 ,  C07C251/48 ,  C07D233/54 ,  C07D233/90

CPC分类号： C07D233/54 ,  C07C251/48 ,  C07C45/63 ,  C07D233/90

摘要： A process for producing 1-substituted-2-cyanoimidazole compounds is described, which comprises (1) undergoing a reaction of a compound represented by formula (IV), hydroxylamine or a mineral acid salt thereof, and glyoxal or glyoxime to produce a compound represented by formula (III), (2) undergoing a reaction of the compound represented by formula (III) with thionyl chloride or thionyl bromide in the presence of N,N-dialkylamide to produce a reaction mixture, and then reacting the produced reaction mixture with sulfur chloride to produce a 2-cyanoimidazole compound represented by formula (II), and (3) undergoing a sulfamoylation reaction and an isomerization reaction of the 2-cyanoimidazole compound represented by formula (II) and a compound represented by formula (V) in the presence of at least one base selected from carbonates of alkali metals and bicarbonates of alkali metals and a polar solvent to produce a 1-substituted-2-cyanoimidazole compound represented by formula (I-b). The formulae and substituents formulae are specifically defined in the specification. ##STR1##

摘要翻译： 描述了一种制备1-取代-2-氰基咪唑化合物的方法，其包括（1）进行由式（Ⅳ）表示的化合物，羟胺或其无机酸盐与乙二醛或乙肟的反应，以制备代表 通过式（III），（2）在N，N-二烷基酰胺存在下，将由式（III）表示的化合物与亚硫酰氯或亚硫酰溴反应生成反应混合物，然后使所产生的反应混合物与 制备由式（II）表示的2-氰基咪唑化合物，和（3）进行氨基甲酰化反应和由式（II）表示的2-氰基咪唑化合物和式（V）表示的化合物的异构化反应在 存在选自碱金属和碱金属的碳酸氢盐的碳酸盐和极性溶剂的至少一种碱，以制备由式（Ib）表示的1-取代-2-氰基咪唑化合物。 式和取代基式在本说明书中具体定义。 （四）