51111-52-5Relevant academic research and scientific papers
Cu(I)-Catalyzed Intramolecular Tandem Cyclization of N-Indole-Tethered Cyclopropenes: Synthesis of Functionalized Hydrogenated Diazabenzo[ a]cyclopenta[ cd]azulene Derivatives
Li, Peng-Hua,Yang, Song,Hao, Tong-Gang,Xu, Qin,Shi, Min
, (2019)
A Cu(I)-catalyzed [3 + 2] intramolecular cycloaddition reaction of N-indole-tethered cyclopropenes is presented in this paper. This reaction starts from the formation of ?-allyl cationic intermediate or its resonance-stabilized metal carbenoid intermediate upon activation of cyclopropene with Cu(I) catalyst and a Friedel-Crafts-type cyclization to give functionalized hydrogenated diazabenzo[a]cyclopenta[cd]azulenes in good to excellent yields along with moderate to good dr values. The asymmetric variant of this cycloaddition reaction can be realized, giving the desired products with moderate ee values.
Design, synthesis and biological evaluation of novel chiral oxazino-indoles as potential and selective neuroprotective agents against Aβ25–35-induced neuronal damage
Chen, Jing,Tao, Ling-Xue,Xiao, Wei,Ji, Sha-Sha,Wang, Jian-Rong,Li, Xu-Wen,Zhang, Hai-Yan,Guo, Yue-Wei
, p. 3765 - 3769 (2016/07/22)
A series of chiral oxazino-indoles have been synthesized via a key intermolecular oxa-Pictet–Spengler reaction. These compounds exhibited significant and selective neuroprotective effects against Aβ25–35-induced neuronal damage. This is the first report of evaluating the influence of chiral diversity of oxazino-indoles on their neuroprotective activities, with the structure–activity relationship been analyzed. The highly active compounds 3f, 3g, 4g, 4h, and 6b all performed over 90% cell protection, providing a new direction for the development of neuroprotective agents against Alzheimer's disease.
