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1.发明公开PROCESSES AND INTERMEDIATES FOR PREPARING 3-(1-PIPERAZINYL)-1,2-BENZISOTHIAZOLE 失效过程和中间产物3-（1-哌嗪基）-1,2-苯并异噻唑THE PRODUCTION
公开(公告)号：EP0874834A1
公开(公告)日：1998-11-04
申请号：EP96931940.0
申请日：1996-10-11
申请人： PFIZER INC.
CPC分类号： C07D275/04 , C07D295/26
摘要： The present invention relates to processes for the preparation of 3-(1-piperazinyl)-1,2-benzisothiazole or its pharmaceutically acceptable salt and to novel intermediates used in the process. 3-(1-piperazinyl)-1,2-benzisothiazole is a key intermediate useful for the preparation of ziprasidone.
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2.发明公开PROCESS AND INTERMEDIATES FOR PREPARING NAPHTHYRIDONECARBOXYLIC ACID SALTS 失效过程和中间产品用于制备naphthyridonecarboxylic酸盐
公开(公告)号：EP0740667A1
公开(公告)日：1996-11-06
申请号：EP95901569.0
申请日：1994-12-12
申请人： PFIZER INC.
CPC分类号： C07D471/04
摘要： This invention relates to novel processes for preparing compounds of formula (I), wherein R1H is as defined below, which is a salt of the naphthyridone antibiotic 7-(1α,5α,6α)-(6-amino-3-azabicyclo[3.1.0]hex-3-yl)-1-(2,4-difluorophenyl)-6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carbocylic acid and a pharmaceutically acceptable acid. The salt and antibiotics have antibacterial activity. This invention also relates to novel intermediates, and processes for their preparation, of formulae (IV), (IIIB) or (IIIA). The compounds of formulae (IIIA), (IIIB) and (IV) are useful as intermediates in the syntheses of the azabicyclo naphthyridone carboxylic acid alkanesulfonic acid salts of formula (I).
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3.发明授权PROCESSES AND INTERMEDIATES FOR PREPARING 3-(1-PIPERAZINYL)-1,2-BENZISOTHIAZOLE 失效过程和中间产物3-（1-哌嗪基）-1,2-苯并异噻唑THE PRODUCTION
公开(公告)号：EP0874834B1
公开(公告)日：2000-12-13
申请号：EP96931940.9
申请日：1996-10-11
申请人： PFIZER INC.
IPC分类号： C07D275/04 , C07D295/22
CPC分类号： C07D275/04 , C07D295/26
摘要： The present invention relates to processes for the preparation of 3-(1-piperazinyl)-1,2-benzisothiazole or its pharmaceutically acceptable salt and to novel intermediates used in the process. 3-(1-piperazinyl)-1,2-benzisothiazole is a key intermediate useful for the preparation of ziprasidone.
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