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1. 发明授权

US5438150A Process for making 1-benzocycloalkyl-1,3-dihydroimidazole-2-thione derivatives 失效
标题翻译：制备1-苯并环烷基-1,3-二氢咪唑-2-硫酮衍生物的方法
公开(公告)号：US5438150A
公开(公告)日：1995-08-01
申请号：US233655
申请日：1994-04-26
申请人： Rekha P. Bansal , Owen W. Gooding , Alexander V. Muehldorf , Counde O-Yang
发明人： Rekha P. Bansal , Owen W. Gooding , Alexander V. Muehldorf , Counde O-Yang
IPC分类号： C07D233/28 , C07D233/32 , C07D233/36 , C07D233/42 , C07D233/60 , C07D233/84 , C07D249/12 , C07D403/04 , C07D403/10 , C07D405/12 , C07C231/08
CPC分类号： C07D403/04 , C07D233/28 , C07D233/32 , C07D233/36 , C07D233/42 , C07D233/84 , C07D249/12 , C07D403/10 , C07D405/12 , Y02P20/582
摘要： The present invention relates to a process for preparing a 5-(N-substituted)aminomethyl-1-benzocycloalkyl-1,3-dihydroimidazole-2-thione (wherein the N-substituent is selected from formyl, aminocarbonyl, (C.sub.1-4)alkylcarbonyl or trifluoro (C.sub.1-4)alkylcarbonyl), which process comprises reacting a benzocycloalkylamine with thiocyanic acid and dihydroxyacetone to give a corresponding 5-hydroxymethyl-1-benzocycloalkyl-1,3-dihydroimidazole-2-thione and then reacting the 5-hydroxymethyl-1-benzocycloalkyl-1,3-dihydroimidazole-2-thione with a compound of the formula H.sub.2 NC(0)R.sup.2 in which R.sup.2 is hydrogen, amino, (C.sub.1-4)alkyl or trifluoro(C.sub.1-4)alkyl or with an ammonium salt of the formula NH.sub.4.sup.+ - OC(0)R.sup.3 in which R.sup.3 is hydrogen, (C.sub.1-4)alkyl or trifluoro(C.sub.1-4)alkyl.The present invention also relates to a process for preparing 5-aminomethyl-1-benzocycloalkyl-1,3-dihydroimidazole-2-thiones, which process comprises preparing a 5-(N-substituted)aminomethyl-1-benzocycloalkyl-1,3-dihydroimidazole-2-thione (wherein the N-substituent is selected from formyl, (C.sub.1-4)alkylcarbonyl or trifluoro(C.sub.1-4)alkylcarbonyl) by the process described above and then hydrolyzing with acid.
摘要翻译：本发明涉及一种制备5-（N-取代的）氨基甲基-1-苯并环烷基-1,3-二氢咪唑-2-硫酮的方法（其中N-取代基选自甲酰基，氨基羰基，（C1-4）烷基羰基或三氟（C 1-4）烷基羰基），该方法包括使苯并环烷基胺与硫氰酸和二羟基丙酮反应，得到相应的5-羟甲基-1-苯并环烷基-1,3-二氢咪唑-2-硫酮，然后使5-羟甲基 -1-苯并环烷基-1,3-二氢咪唑-2-硫酮与式H2NC（O）R2的化合物反应，其中R 2是氢，氨基，（C 1-4）烷基或三氟（C 1-4）烷基或与式NH 4 + -OC（O）R 3的铵盐，其中R 3是氢，（C 1-4）烷基或三氟（C 1-4）烷基。本发明还涉及一种制备5-氨基甲基-1-苯并环烷基-1,3-二氢咪唑-2-硫杂的方法，该方法包括制备5-（N-取代的）氨基甲基-1-苯并环烷基-1,3- 二氢咪唑-2-硫酮（其中N-取代基选自甲酰基，（C 1-4）烷基羰基或三氟（C 1-4）烷基羰基），然后用酸水解。

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