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OPTICALLY ACTIVE, HETEROAROMATIC beta;-HYDROXY ESTERS, PROCESSES FOR THEIR PREPARATION FROM beta;-KETO ESTERS AND PROCESSES FOR THE PREPARATION OF THESE beta;-KETO ESTERS
OPTICALLY ACTIVE, HETEROAROMATIC beta;-HYDROXY ESTERS, PROCESSES FOR THEIR PREPARATION FROM beta;-KETO ESTERS AND PROCESSES FOR THE PREPARATION OF THESE beta;-KETO ESTERS
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机译:光学活性,杂芳族β;-羟基酯,由其制备β-酮基酯的方法及这些β;-酮基酯的制备方法
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摘要
The present invention relates to optically active heteroaromatic beta -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). ® KIPO & WIPO 2007
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