公开(公告)号：US5227486A

公开(公告)日：1993-07-13

申请号：US847625

申请日：1992-03-06

Applicant: Ramon Merce-Vidal ,  Jordi Frigola-Constansa ,  Juan Pares-Corominas

Inventor： Ramon Merce-Vidal ,  Jordi Frigola-Constansa ,  Juan Pares-Corominas

IPC: A61K31/40 ,  A61K31/435 ,  A61K31/495 ,  A61K31/496 ,  A61K31/505 ,  A61P9/12 ,  A61P25/00 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  C07D207/32 ,  C07D207/325 ,  C07D231/12 ,  C07D231/16 ,  C07D231/20 ,  C07D231/38 ,  C07D231/56 ,  C07D233/61 ,  C07D233/68 ,  C07D239/26 ,  C07D241/04 ,  C07D277/64 ,  C07D403/12 ,  C07D403/14 ,  C07D417/12 ,  C07D471/04 ,  C07D521/00

CPC classification number: C07D207/325 ,  C07D231/12 ,  C07D231/16 ,  C07D233/56 ,  C07D233/68 ,  C07D249/08 ,  C07D403/12 ,  C07D403/14 ,  C07D417/12 ,  C07D471/04

Abstract: The present invention relates to a process for the preparation of aryl (or heteroaryl) piperazinyl-butylazole derivatives corresponding to the general formula I ##STR1## in which Ar denotes a nitrogenous or other aromatic radical chosen from differently substituted aryls, differently substituted 2-pyrimidine, 2-N-methyl-imidazole and 3-(1,2-benzisothiazole)Z.sub.1 denotes a nitrogen atom or an optionally substituted carbon atom which may be denoted by: C-R.sub.1Z.sub.2 denotes a nitrogen atom or an optionally substituted carbon atom which may be denoted by: C-R.sub.2Z.sub.4 denotes a nitrogen atom or an optionally substituted carbon atom which may be denoted by: C-R.sub.4 and R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which are identical or different and may also form a part of another ring, aromatic or otherwise, denote a hydrogen atom, a halogen, a lower alkyl radical, a nitro radical, a hydroxyl radical, an alkoxy radical, a cyano radical, a carboxylic radical, a carboxamido radical, an alkylcarboxylate radical, an aryl or substituted aryl radical, a sulfonic radical, a sulfonamido radical optionally substituted on the amino group or an amino or substituted amino radicalwherein ##STR2## in which Ar has the meanings referred to above and X denotes a halogen atom, is reacted with a compound of general formula III ##STR3## in which Z.sub.1, Z.sub.2, Z.sub.4 and R.sub.3 have the meanings referred to above.

Abstract translation: 本发明涉及一种制备相应于通式I（I）的芳基（或杂芳基）哌嗪基 - 丁唑衍生物的方法，其中Ar表示选自不同取代的芳基的含氮或其它芳族基团， 2-嘧啶，2-N-甲基咪唑和3-（1,2-苯并异噻唑）Z1表示氮原子或任选取代的碳原子，可以用以下表示：C-R 1 Z 2表示氮原子或任选取代的 碳原子，其可以由以下表示：C-R 2 Z 4表示氮原子或任选取代的碳原子，其可以由以下表示：C-R 4和R 1，R 2，R 3和R 4，其相同或不同，并且也可以形成 另一个芳环或其它环的一部分表示氢原子，卤素，低级烷基，硝基，羟基，烷氧基，氰基，羧基，甲酰胺基，烷基羧酸根， 芳基或取代基 在氨基或氨基或取代的氨基上任选取代的磺酰基，磺酰氨基，其中Ar具有上述含义，X表示卤素原子的氨基或取代的氨基，与其反应，与 其中Z1，Z2，Z4和R3具有上述含义的通式III的化合物（III）。