发明公开
EP2113031A1 OPTICALLY ACTIVE, HETEROAROMATIC BETA-HYDROXY ESTERS, PROCESSES FOR THEIR PREPARATION FROM BETA-KETO ESTERS AND PROCESSES FOR THE PREPARATION OF THESE BETA-KETO ESTERS
审中-公开
旋光,杂β-羟基酯,METHOD FORβ-酮酯的呈现,AND METHOD FOR DISPLAYING THISβ-酮酯
- 专利标题: OPTICALLY ACTIVE, HETEROAROMATIC BETA-HYDROXY ESTERS, PROCESSES FOR THEIR PREPARATION FROM BETA-KETO ESTERS AND PROCESSES FOR THE PREPARATION OF THESE BETA-KETO ESTERS
- 专利标题(中): 旋光,杂β-羟基酯,METHOD FORβ-酮酯的呈现,AND METHOD FOR DISPLAYING THISβ-酮酯
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申请号: EP04804342.6申请日: 2004-12-21
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公开(公告)号: EP2113031A1公开(公告)日: 2009-11-04
- 发明人: KLAR, Ulrich , PLATZEK, Johannes , ZORN, Ludwig , BUCHMANN, Bernd , SKUBALLA, Werner , PETROV, Orlin
- 申请人: Bayer Schering Pharma Aktiengesellschaft
- 申请人地址: Müllerstrasse 178 13353 Berlin DE
- 专利权人: Bayer Schering Pharma Aktiengesellschaft
- 当前专利权人: Bayer Schering Pharma Aktiengesellschaft
- 当前专利权人地址: Müllerstrasse 178 13353 Berlin DE
- 优先权: DE10361794 20031231
- 国际公布: WO2005064006 20050714
- 主分类号: C12P41/00
- IPC分类号: C12P41/00 ; C07D215/14 ; C07D217/16 ; C07D235/06 ; C07D263/56 ; C07D277/64 ; C07D277/62
摘要:
The present invention relates to optically active heteroaromatic β -hydroxy esters of formula (I) useful in the synthesis of epothilone derivatives, to beta-keto esters of formula (IV) used to produce these intermediates by means of an asymmetric hydrogenation with a chiral metal catalyst or microbiological or enzymatic reduction, as well as to processes for their production (I), wherein: A is a bicyclic heteroaromatic residue of formula (A), wherein “heteroaromatic” stands for a 5-or 6-membered heteroaromatic ring having up to 2 heteroatoms selected from oxygen, nitrogen or sulphur, which is optionally substituted with one or two substituents selected from alkyl, optionally protected hydroxyalkyl, halo-alkyl, halogen or CN, and R is a straight-chain or branched, optionally saturated alkyl chain, which optionally contains 1-3 oxygen atoms; phenyl: cyclohexyl; or benzyl residue (IV).
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