School of Chemistry, University of Hyderabad , Hyderabad 500046, India.
Org Lett. 2017 Oct 20;19(20):5665-5668. doi: 10.1021/acs.orglett.7b02824. Epub 2017 Oct 6.
The methylphenyl sulfoximine (MPS) directing group (DG) successfully promotes the one-pot double annulation of acrylic acids with alkynes under Ru catalysis, which is unprecedented. Diverse arrays of pyrido-fused-isoquinolinone skeletons are fabricated from acrylamides, creating two C-C and two C-N bonds in a single operation. The unsymmetrical annulation with two distinct alkynes is presented. The recovery of methylphenyl sulfoxide, a precursor of MPS, validates the synthetic adaptability of transformable-DG (TDG) in C-H activation.
甲基苯基亚砜（MPS）导向基团（DG）在 Ru 催化下成功促进了丙烯酸与炔烃的一锅双环化反应，这是前所未有的。从丙烯酰胺出发，制备了多种吡啶并稠合异喹啉酮骨架，在单一操作中构建了两个 C-C 和两个 C-N 键。展示了具有两个不同炔烃的不对称环化反应。MPS 的前体甲基苯基亚砜的回收验证了可转化-DG（TDG）在 C-H 活化中的合成适应性。
