Department of Chemistry, National University of Singapore, 3 Science Drive 3, Singapore 117543, Singapore.
J Am Chem Soc. 2010 Nov 10;132(44):15474-6. doi: 10.1021/ja1048972.
A novel amino-thiocarbamate-catalyzed bromolactonization of unsaturated carboxylic acids has been developed. The scope of the reaction is evidenced by 22 examples of γ-lactones with up to 99% yield and 93% ee. The protocol was applied in the enantioselective synthesis of the key intermediates of VLA-4 antagonists.
一种新型的氨基酸硫代氨基甲酸盐催化不饱和羧酸的溴内酯化反应已经被开发出来。该反应的范围由 22 个 γ-内酰胺的例子证明，产率高达 99%，ee 值高达 93%。该方案被应用于 VLA-4 拮抗剂关键中间体的对映选择性合成中。
