An efficient and scalable synthesis of (2R,αS)‐3,4‐dihydro‐2‐[3‐(1,1,2,2‐tetrafluoroethoxy)phenyl]‐5‐[3‐(trifluoromethoxy)phenyl]‐α‐(trifluoromethyl)‐1(2H)‐quinolineethanol: A potent CETP inhibitor
摘要：
An efficient and scalable synthesis of the potent CETP inhibitor, (2R,S)-3,4-dihydro-2-[3-(1,1,2,2-tetrafluoroethoxy)phenyl]-5-[3-(trifluoromethoxy)phenyl]--(trifluoromethyl)-1(2H)-quinolineethanol 1, is described. One of the important intermediates, tetrahydroquinoline 10, was readily prepared by reductive cyclization of nitroketone 9 in high yield. Asymmetric synthesis of 10 with high enantiomeric excess (<80% ee) was also developed. J. Heterocyclic Chem., (2010).
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关键词：
quinoline derivatives ring closure reactions diastereoselective syntheses, enantioselective syntheses (incl. cis/trans-isomerism
DOI：
10.1002/jhet.488
年份：
2010
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