Department of Chemistry, Indian Institute of Technology , Kanpur 208016, India.
Department of Chemistry, Government College for Women , Mandya 571401, Karnataka India.
J Org Chem. 2016 Aug 5;81(15):6433-43. doi: 10.1021/acs.joc.6b01551. Epub 2016 Jul 25.
Lewis acid catalyzed domino ring-opening cyclization of activated aziridines with aryl and alkyl isothiocyanates has been accomplished leading to the formation of a wide variety of highly substituted and functionalized 2-iminothiazolidines with excellent diastereo- and enantiospecificity (de, ee up to >99%). The reaction proceeds via a Lewis acid catalyzed SN2-type ring-opening of the activated aziridine followed by a concomitant 5-exo-dig cyclization in a domino fashion to furnish the 2-iminothiazolidine derivative in excellent yields (up to 99%).
路易斯酸催化的活化氮丙啶与芳基和烷基异硫氰酸酯的串联开环环化反应已经完成，生成了各种高度取代和官能化的 2-亚氨基噻唑烷，具有优异的非对映选择性和对映选择性（de，ee 高达>99%）。该反应通过路易斯酸催化的活化氮丙啶的 SN2 型开环，随后以串联方式进行同时的 5-endo-环化，以高产率（高达 99%）得到 2-亚氨基噻唑烷衍生物。
