尿素衍生催化剂促进的羟吲哚与色酮的对映选择性羟烷基化反应。
Urea-Derivative Catalyzed Enantioselective Hydroxyalkylation of Hydroxyindoles with Isatins.
机构信息
Department of Pharmacy, Jilin Medical University, Jilin, Jilin 132013, China.
出版信息
Molecules. 2019 Oct 31;24(21):3944. doi: 10.3390/molecules24213944.
The enantioselective transformations of indoles preferentially take place in the more-reactive azole ring. However, the methods for the enantioselective functionalization of the indole benzene ring are scarce. In this paper, a series of bifunctional (thio)urea derivatives were used to organocatalyze the enantioselective Friedel-Crafts hydroxyalkylation of indoles with isatins. The resulting products were obtained in good yields (65-90%) with up to 94% enantiomer excess (ee). The catalyst type and the substrate scope were broadened in this methodology.
吲哚的对映选择性转化优先发生在更具反应性的唑环上。然而，吲哚苯环的对映选择性官能化方法却很少。在本文中，一系列双功能（硫）脲衍生物被用于有机催化吲哚与靛红的对映选择性Friedel-Crafts 羟烷基化反应。所得产物的产率（65-90%）较高，对映体过量（ee）高达 94%。该方法拓宽了催化剂类型和底物范围。
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