作者:Kizhakkan Thiruthi Ashitha、Puthiya Purayil Vinaya、Ajay Krishna、Deepthy Cheeran Vincent、Renjitha Jalaja、Sunil Varughese、Sasidhar Balappa Somappa
DOI:10.1039/c9ob02711d
日期:——
spiroheterocycles are considered as emerging drug candidates, synthesis of spiroaziridines has not been well explored so far. Herein, we disclose an efficient I2/TBHP mediated diastereoselective synthesis of N-alkyl spiroaziridines from primary amines and easily accessible α,β-unsaturated ketones. The reaction is also compatible for the synthesis of 2-aroylaziridines.
尽管螺杂环被认为是新兴的候选药物,但迄今为止螺氮丙啶的合成还没有得到很好的探索。在此,我们公开了一种有效的 I2/TBHP 介导的非对映选择性合成 N-烷基螺氮丙啶,从伯胺和易于获得的 α,β-不饱和酮。该反应也适用于 2-芳酰基氮丙啶的合成。