发明公开
- 专利标题: METHODS FOR THE PREPARATION OF BENZOXAZOLE SULFONAMIDE COMPOUNDS AND INTERMEDIATES THEREOF
- 专利标题(中): 用于生产恶唑磺酰胺化合物及其中间体的
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申请号: EP04766869.4申请日: 2004-09-30
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公开(公告)号: EP1670773A1公开(公告)日: 2006-06-21
- 发明人: DE KOCK, Herman Augustinus , FILLIERS, Walter Ferdinand Maria , AELTERMAN, Wim Albert Alex
- 申请人: Tibotec Pharmaceuticals Ltd.
- 申请人地址: Little Island Co Cork IE
- 专利权人: Tibotec Pharmaceuticals Ltd.
- 当前专利权人: Tibotec Pharmaceuticals Ltd.
- 当前专利权人地址: Little Island Co Cork IE
- 代理机构: Daelemans, Frank F.R.
- 优先权: EP03103630 20030930; US507996P 20031002
- 国际公布: WO2005030739 20050407
- 主分类号: C07D263/58
- IPC分类号: C07D263/58
摘要:
The present invention relates to methods for the preparation of benzoxazole sulfonamide compounds of formula (9) as well as novel intermediates of formula (6) for use in said method. More in particular the invention relates to methods for the Preparation of 2-amino-benzoxazole sulfonamide compounds which make use of 2-mercapto-benzoxazole sulfonamide intermediates, more in particular methods employing the intermediate 1-Benzy1-2-hydroxy-3-[isobutyl(2-methylsulfanyl-benzoxazole-6-sulfonyl)-amino)-propyl)-carbamic ester, and to methods amenable to industrial scaling up. Said benzoxazole sulfonamide compounds are particularly useful as HIV protease inhibitors. The substituents are defined in the claims.
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