摘要/Abstract

含噻吩基团的的手性芳香醇是自然界重要的活性物质，其基本结构单元广泛地存在于生物活性物质和医药中.报道了（S）-联萘酚和Ti（OⁱPr）₄催化3-噻吩基铝试剂对酮的不对称加成反应，以较高的产率和优异的立体选择性（高达91%ee）得到相应的含有3-噻吩基乙醇.该催化体系具有广泛的适应性，能够适合含有吸电子和供电子基团的各种酮的不对称加成，得到相应的3-噻吩基乙醇.
关键词: 不对称合成, 噻吩基, 铝试剂, 钛, 酮
The optically active diaryl alcohols bearing thienyl group are well-known for their biological activity as well as key substructure in bioactive compounds and pharmaceuticals. The asymmetric addition of 3-thienyl aluminum to ketones afforded the optically active 3-thienyl arylethanols in good yields with high enantioselectivities of up to 91% ee employing the simple titanium catalytic system of (S)-1,1'-binaphthol. The catalytic system could also suit for various ketones bearing an electron-donating or electron-withdrawing groups to afford the corresponding diarylethanols containing substituted 3-thienyl groups.
Key words: asymmetric synthesis, thienyl, aluminum, titanium, ketones


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