发明公开
EP2565179A1 Reagents and methods for the beta-keto amide synthesis of a synthetic precursor to immunological adjuvant e6020
审中-公开
试剂和方法免疫Ajduvans E6020的合成前体的β-酮酰胺合成
- 专利标题： Reagents and methods for the beta-keto amide synthesis of a synthetic precursor to immunological adjuvant e6020
- 专利标题（中）： 试剂和方法免疫Ajduvans E6020的合成前体的β-酮酰胺合成
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申请号： EP12178716.2申请日： 2008-12-18
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公开(公告)号： EP2565179A1公开(公告)日： 2013-03-06
- 发明人: Decosta, Bruce , Fang, Francis, G. , Foy, James, E. , Hawkins, Lynn , Lemelin, Charles , Niu, Xiang , Wu, Kuo-Ming
- 申请人： Eisai R&D Management Co., Ltd.
- 申请人地址： 6-10, Koishikawa 4-chome, Bunkyo-ku Tokyo 112-8088 JP
- 专利权人： Eisai R&D Management Co., Ltd.
- 当前专利权人： Eisai R&D Management Co., Ltd.
- 当前专利权人地址： 6-10, Koishikawa 4-chome, Bunkyo-ku Tokyo 112-8088 JP
- 代理机构： Jewell, Catherine Mary
- 优先权： US14648P 20071218
- 主分类号： C07C235/70
- IPC分类号： C07C235/70 ; C07C231/00 ; C07F9/24 ; C07C235/74 ; C07C235/76
摘要：
This invention relates to the synthesis for a precursor of E6020, compound 26, via a β-keto amide alcohol intermediate, compound 22. The synthesis reacts compound 22 with compound 25 and the resultant intermediate is oxidized to produce compound 26, the precursor to E6020. Compounds 22 and 25, and their crystalline forms, represent separate embodiments of the invention. The invention also relates to compounds of formulas (3) and (4) and processes for their preparation. The β-keto amide alcohol intermediate compound 22 is a compound of formula (3). Compound 25 is a compound of formula (4).
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