发明申请
US20050101583A1 Process and intermediates for the production of 7-substituted antiestrogens
有权
用于生产7-取代的抗雌激素的方法和中间体
- 专利标题: Process and intermediates for the production of 7-substituted antiestrogens
- 专利标题(中): 用于生产7-取代的抗雌激素的方法和中间体
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申请号: US10398924申请日: 2001-10-09
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公开(公告)号: US20050101583A1公开(公告)日: 2005-05-12
- 发明人: Robert Stevenson , Fraser Kerr , Anthony Lane , Eve Brazier , Philip Hogan , David Laffan
- 申请人: Robert Stevenson , Fraser Kerr , Anthony Lane , Eve Brazier , Philip Hogan , David Laffan
- 申请人地址: SE Sodertalje
- 专利权人: AstraZeneca AB
- 当前专利权人: AstraZeneca AB
- 当前专利权人地址: SE Sodertalje
- 优先权: GB0025221.3 20001014
- 国际申请: PCT/GB01/04485 WO 20011009
- 主分类号: C07B61/00
- IPC分类号: C07B61/00 ; C07J31/00 ; C07J41/00 ; C07J75/00 ; A61K31/56 ; C07J1/00
摘要:
A process for preparing an intermediate compound of formula (II) where X is as defined in the specification, R1 is haloalkyl, alkyl, alkenyl, cycloalkyl, carboxyalkyl, alkoxycarbonylalkyl, aryl or arylalkyl; R2, R3, R4 and R5 are organic groups as defined in the specification, which process comprises aromatisation of a compound of formula (III) where R1, R2, R3, n, X and R5 are as defined in relation to formula (II) and R4′ is a group R4 or a precursor group thereof, and thereafter if necessary or desired, carrying out one or more of the following steps: (i) removing any hydroxy-protecting groups R; (ii) converting a precursor group R4′ to a group R4, or where R4′ is a group R4, converting it to a different such group. Compounds obtained are useful intermediates for example in the preparation of fulvestrant. Novel intermediates are also claimed.
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