Enantioselective Synthesis of 1-Aryl-tetrahydroisoquinolines through Iridium Catalyzed Asymmetric Hydrogenation
Enantioselective Synthesis of 1-Aryl-tetrahydroisoquinolines through Iridium Catalyzed Asymmetric Hydrogenation
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DOI：
10.1021/ol301281s
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发表时间：
2012-07-06
期刊：
影响因子：
5.2
通讯作者：
Ratovelomanana-Vidal, Virginie
中科院分区：
文献类型：
--
作者：
Berhal, Farouk;Wu, Zi;Ratovelomanana-Vidal, Virginie
报道了1-芳基-3，4-二氢异喹啉在[IrCODCl](2)/(R)-3，5-二甲基-Synphos催化剂上的不对称加氢反应。在温和的反应条件下，这种原子经济的方法可以很容易地获得各种富含对映体的1-芳基-1，2，3，4-四氢异喹啉衍生物，这些衍生物是几种候选药物中的重要药效团，高产率，一次结晶后对映体过量高达99%。
Asymmetric hydrogenation of 1-aryl-3,4-dihydrolsoquinolines using the [IrCODCl](2)/(R)-3,5-diMe-Synphos catalyst is reported. Under mild reaction conditions, this atom-economical process provides easy access to a variety of enantioenriched 1-aryl-1,2,3,4-tetrahydroisoquinoline derivatives, which are important pharmacophores found in several pharmaceutical drug candidates, in high yields and enantiomeric excesses up to 99% after a single crystallization.