Highly Enantioselective Rhodium-Catalyzed Addition of Arylboroxines to Simple Aryl Ketones: Efficient Synthesis of Escitalopram
Highly Enantioselective Rhodium-Catalyzed Addition of Arylboroxines to Simple Aryl Ketones: Efficient Synthesis of Escitalopram
复制标题
高对映选择性铑催化芳基环硼氧烷与简单芳基酮的加成：艾司西酞普兰的高效合成
DOI：
10.1002/anie.201600979
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发表时间：
2016-03-24
影响因子：
16.6
通讯作者：
Tang, Wenjun
中科院分区：
文献类型：
--
作者：
Huang, Linwei;Zhu, Jinbin;Tang, Wenjun
首次在Rh/（R，R，R，R）-WingPhos催化剂上实现了芳基环硼氧烷与简单芳基酮的高对映选择性加成反应，从而以优异的评价和产率合成了一系列手性二芳基烷基甲醇。（R，R，R，R）-WingPhos被证明是高反应活性和对映选择性的关键。该方法使抗抑郁药艾司西酞普兰的新的、简洁的和对映选择性的合成成为可能。
Highly enantioselective additions of arylboroxines to simple aryl ketones have been achieved for the first time with a Rh/(R,R,R,R)-WingPhos catalyst, thus providing a range of chiral diaryl alkyl carbinols with excellent eevalues and yields. (R,R,R,R)-WingPhos has been proven to be crucial for the high reactivity and enantioselectivity. The method has enabled a new, concise, and enantioselective synthesis of the antidepressant drug escitalopram.