[3 + 2] Cycloaddition of α-Aryl-α-diazoacetates with Terminal Alkynes via the Cooperative Catalysis of Palladium and Acid

ACS Catalysis ◽  
2021 ◽  
pp. 10789-10795
Author(s):  
Hongyu Guo ◽  
Sheng Zhang ◽  
Xiaoqiang Yu ◽  
Xiujuan Feng ◽  
Yoshinori Yamamoto ◽  
...  
2017 ◽  
Vol 53 (17) ◽  
pp. 2606-2609 ◽  
Author(s):  
Chuan Zhu ◽  
Chao Feng ◽  
Motoki Yamane

We report a cooperative Pd/Cu-catalyzed synthesis of (3-isoindazolyl)allenes via cross-coupling of 2-alkynyl azobenzenes and terminal alkynes.


2020 ◽  
Vol 16 ◽  
Author(s):  
Lucas da Silva Santos ◽  
Matheus Fillipe Langanke de Carvalho ◽  
Ana Claudia de Souza Pinto ◽  
Amanda Luisa da Fonseca ◽  
Julio César Dias Lopes ◽  
...  

Background: Malaria greatly affects the world health, having caused more than 228 million cases only in 2018. The emergence of drug resistance is one of the main problems in its treatment, demonstrating the urge for the development of new antimalarial drugs. Objective: Synthesis and in vitro antiplasmodial evaluation of triazole compounds derived from isocoumarins and a 3,4- dihydroisocoumarin. Method: The compounds were synthesized in 4 to 6-step reactions with the formation of the triazole ring via the Copper(I)-catalyzed 1,3-dipolar cycloaddition between isocoumarin or 3,4-dihydroisocoumarin azides and terminal alkynes. This key reaction provided compounds with an unprecedented connection of isocoumarin or 3,4-dihydroisocoumarin and the 1,2,3-triazole ring. The products were tested for their antiplasmodial activity against a Plasmodium falciparum chloroquine resistant and sensitive strains (W2 and 3D7, respectively). Results: Thirty-one substances were efficiently obtained by the proposed routes with an overall yield of 25-53%. The active substances in the antiplasmodial test displayed IC50 values ranging from 0.68-2.89 μM and 0.85-2.07 μM against W2 and 3D7 strains, respectively.


2015 ◽  
Vol 48 (7) ◽  
pp. 2140-2150 ◽  
Author(s):  
Florian Klappenberger ◽  
Yi-Qi Zhang ◽  
Jonas Björk ◽  
Svetlana Klyatskaya ◽  
Mario Ruben ◽  
...  

2012 ◽  
Vol 53 (41) ◽  
pp. 5559-5561 ◽  
Author(s):  
Xinjiang Niu ◽  
Chunju Li ◽  
Jian Li ◽  
Xueshun Jia

2021 ◽  
Vol 503 ◽  
pp. 111415
Author(s):  
Di Wu ◽  
Qingqing Bu ◽  
Cheng Guo ◽  
Bin Dai ◽  
Ning Liu

Sign in / Sign up

Export Citation Format

Share Document