6260-86-2Relevant articles and documents
Synthesis of Chiral Polycyclic Tetrahydrocarbazoles by Enantioselective Aminocatalytic Double Activation of 2-Hydroxycinnamaldehydes with Dienals
Ming, Yong-Chao,Lv, Xue-Jiao,Liu, Ming,Liu, Yan-Kai
supporting information, p. 6515 - 6519 (2021/09/02)
An efficient aminocatalytic enantioselective double-activation strategy has been developed that combines several different aminocatalytic modes in a cascade process, such as iminium ion, vinylogous iminium ion, trienamine, and dienamine activations. By using this strategy, 2-hydroxycinnamaldehydes worked well with various dienals via [4 + 2] cycloaddition and the oxa-Michael reaction-initiated cascade, respectively, leading to chiral polycyclic tetrahydrocarbazole and chromane derivatives with excellent diastereo- and enantioselectivities.
Evodiamine prodrug containing indole quinone unit as well as preparation method and application thereof
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Paragraph 0017; 0022, (2021/10/30)
The invention relates to an evodiamine prodrug containing an indole quinone unit as well as a preparation method and application thereof. The invention synthesizes a series of strong active evodiamine derivatives with indole quinine units, has strong anti-proliferative activity on non-small cell lung cancer (non-small cell lung cancer, NSCLC), and has dosage and time dependence. In-vitro experiments evaluate their biological activity, suggesting that the synthesized compounds have a strong inhibitory activity on lung cancer strains. Through molecular docking analysis, the binding affinity of the ligand to the active site of the target protein is predicted, and the interaction ability of the ligand and the protein is strong.
Exploiting the Distal Reactivity of Indolyl Methylenemalononitriles: An Asymmetric Organocatalyzed [4+2] Cycloaddition with Enals Enables the Assembly of Elusive Dihydrocarbazoles
Rassu, Gloria,Curti, Claudio,Zambrano, Vincenzo,Pinna, Luigi,Brindani, Nicoletta,Pelosi, Giorgio,Zanardi, Franca
supporting information, p. 12637 - 12640 (2016/08/30)
An unprecedented technique for the in situ generation of indolyl ortho-quinodimethanes from 2-methylindole-based methylenemalononitriles by amine-mediated remote C(sp3)?H deprotonation was developed. These intermediates were efficiently trapped by diverse enals to provide a rapid entry to 2,9-dihydro-1H-carbazole-3-carboxyaldehyde structures through a formal asymmetric [4+2] eliminative cycloaddition governed by a α,α-diphenylprolinol trimethylsilyl ether catalyst.