发明名称 Process and intermediates for the production of 7-substituted antiestrogens
摘要 A process is disclosed for preparing an intermediate compound of formula (II), wherein R is hydrogen or a hydroxy protecting group; 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 pharmaceutical compounds such as fulvestrant.
申请公布号 NZ525096(A) 申请公布日期 2004.10.29
申请号 NZ20010525096 申请日期 2001.10.09
申请人 ASTRAZENECA AB 发明人 STEVENSON, ROBERT;KERR, FRASER WITTON;LANE, ANTHONY RAYMOND;BRAZIER, EVE JOANNE;HOGAN, PHILIP JOHN;LAFFAN, DAVID DERMOT PATRICK
分类号 C07B61/00;C07J31/00;C07J41/00;C07J75/00 主分类号 C07B61/00
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