通过环状亚氨基酯与 Morita-Baylis-Hillman 溴化物的串联反应，催化不对称构建螺（γ-丁内酯-γ-丁内酯）部分。
Catalytic asymmetric construction of spiro(γ-butyrolactam-γ-butyrolactone) moieties through sequential reactions of cyclic imino esters with Morita-Baylis-Hillman bromides.
机构信息
College of Chemistry and Molecular Sciences, Wuhan University, PR China.
出版信息
Chemistry. 2012 Oct 1;18(40):12614-8. doi: 10.1002/chem.201201475. Epub 2012 Aug 27.
PMID:22927370
Abstract
Spiro(γ-butyrolactam-γ-butyrolactone): a route to enantioenriched spiro(γ-butyrolactam-γ-butyrolactone) compounds, a valuable motif for drug discovery, was developed by use of a highly efficient copper(I)/TF-BiphamPhos-catalyzed tandem Michael addition-elimination of homoserine lactone derived cyclic imino esters with Morita-Baylis-Hillman (MBH) bromides, followed by treatment with para-toluenesulfonic acid.
摘要
螺环（γ-丁内酯-γ-丁内酯）：一种用于手性富集螺环（γ-丁内酯-γ-丁内酯）化合物的途径，是药物发现的一个有价值的主题，该方法通过使用高效的铜（I）/TF-BiphamPhos 催化的高丝氨酸内酯衍生的环状亚氨基酯与 Morita-Baylis-Hillman (MBH) 溴化物的串联迈克尔加成-消除反应，然后用对甲苯磺酸处理来实现。
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