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手性二胺金属钌配合物催化不对称氢化合成手性吲哚啉化合物
Highly Enantioselective Synthesis of Indolines via Asymmetric Hydrogenation with Chiral Cationic Ruthenium Diamine Catalysts
【Author】 Fei Chen;Zhusheng Yang;Yanmei He;Qing-Hua Fan;CAS Key Laboratory of Molecular Recognition and Function,Institute of Chemistry,Chinese Academy of Sciences(CAS);
【机构】 中国科学院化学研究所分子识别与功能院重点实验室;
【摘要】 手性吲哚啉化合物是构成各种手性药物或天然生物碱的重要骨架[1]。而吲哚的直接不对称氢化是制备手性吲哚啉化合物最直接和原子经济的方法之一[2]。以手性二胺金属钌配合物为催化剂[3],在常温常压的条件下可以催化一系列1H-吲哚和3H-吲哚衍生物的不对称氢化反应,并取得优异的反应活性(TON高达1000)、对映选择性和非对映选择性(高达>99%ee,>20:1 dr)。
【Abstract】 Optically active indolines are ubiquitous structural moieties in chiral pharmaceuticals and biologically interesting natural alkaloids.[1] Among the various reported methods for attaining optically active indolines,the direct asymmetric hydrogenation of the corresponding readily available indoles represents one of the most straightforward and atom-economic approaches.[2]Herein,we report that a wide range of 1H-indole and 3H-indole derivatives were successfully hydrogenated at ambient temperature and pressure cataylzed by cationic ruthenium diamine catalysts[3] with excellent reactivity(TON up to 1000),enantioselectivity and diastereoselectivity(up to>99%ee,>20:1 dr).
- 【会议录名称】 中国化学会第30届学术年会摘要集-第九分会:有机化学
- 【会议名称】中国化学会第30届学术年会
- 【会议时间】2016-07-01
- 【会议地点】中国辽宁大连
- 【分类号】O626
- 【主办单位】中国化学会