One-Pot Heteroarene Synthesis Based on Ruthenium-on-Carbon-Catalyzed Oxidative Aromatization Using Oxygen

2020 ◽  
Vol 93 (12) ◽  
pp. 1419-1423
Author(s):  
Yuta Yamamoto ◽  
Yutaro Yamada ◽  
Hironao Sajiki ◽  
Yoshinari Sawama
Synthesis ◽  
2018 ◽  
Vol 51 (02) ◽  
pp. 522-529 ◽  
Author(s):  
Deqing Shi ◽  
Lingna Wang ◽  
Tiancong Ma ◽  
Mingming Qiao ◽  
Qiangxian Wu ◽  
...  

A visible-light photoredox-catalyzed oxidation/[3+2] cycloaddition/oxidative aromatization cascade reaction of [(3,4-dihydroisoquinolin-2(1H)-yl)methyl]phosphonates and activated olefins or alkynes for the efficient synthesis of potentially biological active pyrrolo[2,1-a]isoquinoline-substituted phosphonates was developed. This transformation features mild reaction conditions (i.e., visible light irradiation, room temperature), molecular oxygen (O2) as a green oxidant, simple ‘one-pot’ operation.


ChemInform ◽  
2015 ◽  
Vol 46 (20) ◽  
pp. no-no
Author(s):  
Maryam Mirza-Aghayan ◽  
Fatemeh Asadi ◽  
Rabah Boukherroub

2019 ◽  
Vol 21 (17) ◽  
pp. 6879-6883 ◽  
Author(s):  
Miao-Miao Xun ◽  
Yunli Bai ◽  
Yanhong Wang ◽  
Zhiyong Hu ◽  
Kai Fu ◽  
...  

Molbank ◽  
10.3390/m1197 ◽  
2021 ◽  
Vol 2021 (1) ◽  
pp. M1197
Author(s):  
Jasril Jasril ◽  
Neni Frimayanti ◽  
Yuana Nurulita ◽  
Adel Zamri ◽  
Ihsan Ikhtiarudin ◽  
...  

A new fluorinated pyrazole, 5-(4-fluorophenyl)-3-(naphthalen-1-yl)-1-phenyl-1H-pyrazole was successfully synthesized via a two-step reaction. Firstly, the synthesis of pyrazoline was performed via one-pot three-component reaction under microwave irradiation. Secondly, the synthesis of pyrazole was performed via oxidative aromatization of pyrazoline under conventional heating. The structure of the synthesized compound was confirmed by spectroscopic analysis, including FT-IR, HR-MS, 1D and 2D NMR analysis. Then, molecular docking study showed that the binding affinity of the synthesized compound to human estrogen alpha receptor (ERα) was close to 4-OHT as a native ligand.


Molekul ◽  
2020 ◽  
Vol 15 (1) ◽  
pp. 18
Author(s):  
Noval Herfindo ◽  
Riska Prasetiawati ◽  
Daniel Sialagan ◽  
Neni Frimayanti ◽  
Adel Zamri

This research has been successfully synthesized three compounds of 1,3,5-triaryl pyrazole derivatives by two steps reaction. Firstly, pyrazoline (4a-c) compound was obtained by one-pot reaction of aromatic ketones, aldehyde and hydrazine in basic condition. Then, pyrazole (5a-c) compound was obtained by oxidative aromatization of compound 4 in the presense of acetic acid. Chemical structure of predicted molecules was confirmed by FTIR, NMR and HRMS spectroscopy data analysis. Antiproliferative activity of compound 5a-c were evaluated by in vitro assay against MCF-7 cells line and molecular docking simulation against ERα (PDB ID: 3ERT) using MOE 2019. Biological evaluation result showed that pyrazole compounds had weak antiproliferative activity against MCF-7 cells with IC50 were > 1000 µM, whereas the docking studies agrees the result.


Synthesis ◽  
2019 ◽  
Vol 51 (19) ◽  
pp. 3651-3666
Author(s):  
Weiqiang Chen ◽  
Yin-Lin Zhang ◽  
Hui-Jing Li ◽  
Xiang Nan ◽  
Ying Liu ◽  
...  

N-Sulfonyl- and N-acylpyrroles were synthesized via olefin ring-closing metathesis of diallylamines and in situ oxidative aromatization in the presence of the ruthenium Grubbs catalyst and a suitable copper catalyst. In the presence of Cu(OTf)2 and CuBr2, the reaction afforded N-sulfonyl- and N-acylpyrroles, respectively, in one pot. Under an oxygen atmosphere, the reaction went smoothly without the need of hydroperoxide oxidants. This protocol possesses many advantages, such as using a nonhazardous oxidant and readily available starting materials, operating in one pot, and showing a broad substrate scope.


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