亚砜腙辅助的 Rh(III)催化 C-H 活化和分子内环化反应在室温下合成稠合异苯并噻嗪-1,2-并噻嗪骨架。
Sulfoximines-Assisted Rh(III)-Catalyzed C-H Activation and Intramolecular Annulation for the Synthesis of Fused Isochromeno-1,2-Benzothiazines Scaffolds under Room Temperature.
机构信息
State Key Laboratory of Drug Research and CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai 201203, China.
University of Chinese Academy of Sciences, No.19A Yuquan Road, Beijing 100049, China.
出版信息
Molecules. 2020 May 28;25(11):2515. doi: 10.3390/molecules25112515.
A mild and facile Cp*Rh(III)-catalyzed C-H activation and intramolecular cascade annulation protocol has been proposed for the furnishing of highly fused isochromeno-1,2-benzothiazines scaffolds using -phenylsulfoximides and 4-diazoisochroman-3-imine as substrates under room temperature. This method features diverse substituents and functional groups tolerance and relatively mild reaction conditions with moderate to excellent yields. Additionally, retentive configuration of sulfoximides in the conversion has been verified.
提出了一种温和且简便的 Cp*Rh(III)-催化 C-H 活化和分子内级联环化反应方案，使用 -苯亚磺酰胺和 4-重氮异苯并呋喃-3-亚胺作为底物，在室温下合成高度稠合的异色满并[1,2-b]苯并噻嗪骨架。该方法具有多种取代基和官能团的耐受性，以及相对温和的反应条件，产率中等至优秀。此外，在转化过程中验证了亚磺酰胺的保留构型。
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