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

被引：0
作者：
Wang, Aihua [1 ]
Zhang, Yan [1 ]
Lu, Songfeng [1 ]
Murray, William V. [1 ]
Kuo, Gee-Hong [1 ]
机构：
[1] Johnson & Johnson Pharmaceut Res & Dev LLC, Drug Discovery, Spring House, PA 19477 USA
来源：
JOURNAL OF HETEROCYCLIC CHEMISTRY | 2010年 / 47卷 / 06期
关键词：
LIPID TRANSFER PROTEINS; CORONARY-HEART-DISEASE; LIPOPROTEIN CHOLESTEROL; DISCOVERY; REDUCTION; DESIGN;
D O I：
10.1002/jhet.488
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
An efficient and scalable synthesis of the potent CETP inhibitor, (2R,alpha S)-3,4-dihydro-2[3-(,1,2,2-tetrafluoroethoxy)phenyl]-5-[3-(trifluoromethoxy)phenyl]-alpha-(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.
引用
收藏
页码：1406 / 1410
页数：5
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