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Benzo(3,4)cyclobuta(1,2-c)pyrrole derivatives as inhibitors of serotonine reuptake

机译:苯并(3,4)环丁(1,2-c)吡咯衍生物作为5-羟色胺再摄取抑制剂

摘要

cis-Benzo(3,4)cyclobuta(1,2-c)pyrrole derivatives (I) are new. cis-Benzo(3,4)cyclobuta(1,2-c)pyrrole derivatives of formula (I) and their isomers and salts are new. R1 - R3 = H, halogen, 1-6C alkyl, 2-6C alkenyl, 2-6C alkynyl, OH, 1-6C alkoxy, cycloalkyl, cycloalkyl(1-6C)alkyl, aryl, aryl(1-6C)alkyl, aryloxy, aryl(1-6C)alkoxy, 1-6C trihaloalkyl, 1-6C trihaloalkoxy,CN, NO2, OSO2Me, OSO2CF3, NR6R7 or COOR6; or two adjacent R1 - R3 groups = 4-8C optionally saturated ring in which 1-2 C atoms can be replaced by O, N and/or S; R6, R7 = H, 1-6C alkyl, 2-6C alkenyl, 2-6C alkynyl, cycloalkyl, cycloalkyl(1-6C)alkyl, aryl or aryl(1-6C)alkyl; R4 = H, 1-6C alkyl, 2-6C alkenyl, 2-6C alkynyl, cycloalkyl, cycloalkyl(1-6C)alkyl, aryl, aryl(1-6C)alkyl, heterocycloalkyl, heterocycloalkyl(1-6C)alkyl, heteroaryl or heteroaryl(1-6C)alkyl; R5 = aryl or heteroaryl optionally substituted by halogen, OH, 1-6C alkyl, 1-6C alkoxy, 2-6C alkenyl, cycloalkyl, adamantyl, cycloalkyl(1-6C)alkyl, aryl, aryl(1-6C)alkyl, aryloxy, aryl(1-6C)alkoxy, 1-6C trihaloalkyl, CN, NO2, oxo, OSO2Me, OSO2CF3, NR6R7 or COOR6; n = 1 - 3; cycloalkyl = a 3-8C mono- or bicyclic optionally saturated ring system optionally substituted by halogen and/or 1-6C alkyl; heterocycloalkyl = cycloalkyl as defined in which the ring system contains 1-3 heteroatoms selected from O, N and S; aryl = phenyl, naphthyl, dihydronaphthyl, tetrahydronaphthyl, indenyl or indanyl; heteroaryl = aryl as defined containing 1-3 heteroatoms selected from O, N and S. An Independent claim is also included for a process for preparing (I).
机译:顺式(3,4)环丁(1,2-c)吡咯衍生物(I)是新的。式(I)的顺式(3,4)环丁(1,2-c)吡咯衍生物及其异构体和盐是新的。 R1-R3 = H,卤素,1-6C烷基,2-6C烯基,2-6C炔基,OH,1-6C烷氧基,环烷基,环烷基(1-6C)烷基,芳基,芳基(1-6C)烷基,芳氧基,芳基(1-6C)烷氧基,1-6C三卤代烷基,1-6C三卤代烷氧基,CN,NO 2,OSO 2 Me,OSO 2 CF 3,NR 6 R 7或COOR 6;或两个相邻的R 1 -R 3基团= 4-8C,任选为饱和的环,其中1-2个碳原子可被O,N和/或S取代; R6,R7 = H,1-6C烷基,2-6C烯基,2-6C炔基,环烷基,环烷基(1-6C)烷基,芳基或芳基(1-6C)烷基; R4 = H,1-6C烷基,2-6C烯基,2-6C炔基,环烷基,环烷基(1-6C)烷基,芳基,芳基(1-6C)烷基,杂环烷基,杂环烷基(1-6C)烷基,杂芳基或杂芳基(1-6C)烷基; R5 =任选地被卤素,OH,1-6C烷基,1-6C烷氧基,2-6C烯基,环烷基,金刚烷基,环烷基(1-6C)烷基,芳基,芳基(1-6C)烷基,芳氧基取代的芳基或杂芳基,芳基(1-6C)烷氧基,1-6C三卤代烷基,CN,NO2,氧代,OSO2Me,OSO2CF3,NR6R7或COOR6; n = 1-3;环烷基=任选地被卤素和/或1-6C烷基取代的3-8C单环或双环的任选饱和的环系统;杂环烷基=环烷基,其中环系统含有1-3个选自O,N和S的杂原子;芳基=苯基,萘基,二氢萘基,四氢萘基,茚基或茚满基;杂芳基=定义为包含选自O,N和S的1-3个杂原子的芳基。还包括制备(I)的方法的独立权利要求。

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