scholarly journals Mizoroki-Heck Cyclizations of Amide Derivatives for the Introduction of Quaternary Centers

2017 ◽  
Vol 56 (23) ◽  
pp. 6567-6571 ◽  
Author(s):  
Jose M. Medina ◽  
Jesus Moreno ◽  
Sophie Racine ◽  
Shuaijing Du ◽  
Neil K. Garg
Keyword(s):  
Quaternary Centers ◽  
Amide Derivatives

scholarly journals Mizoroki-Heck Cyclizations of Amide Derivatives for the Introduction of Quaternary Centers

2017 ◽  
Vol 129 (23) ◽  
pp. 6667-6671 ◽  
Author(s):  
Jose M. Medina ◽  
Jesus Moreno ◽  
Sophie Racine ◽  
Shuaijing Du ◽  
Neil K. Garg
Keyword(s):  
Quaternary Centers ◽  
Amide Derivatives

Metal-Free Photoinduced Hydroalkylation Cascade Enabled by an Electron-Donor-Acceptor Complex

2020 ◽  
Author(s):  
José Tiago Menezes Correia ◽  
Gustavo Piva da Silva ◽  
Camila Menezes Kisukuri ◽  
Elias André ◽  
Bruno Pires ◽  
...  
Keyword(s):  
Electron Donor ◽  
Functional Group ◽  
Photoexcited Electron ◽  
One Pot ◽  
Quaternary Centers ◽  
Metal Free ◽  
Acceptor Complex ◽  
Catalyst Free ◽  
Donor Acceptor ◽  
Radical Cascade

A metal- and catalyst-free photoinduced radical cascade hydroalkylation of 1,7-enynes has been disclosed. The process is triggered by a SET event involving a photoexcited electron-donor-aceptor complex between NHPI ester and Hantzsch ester, which decomposes to afford a tertiary radical that is readily trapped by the enyne. <a>The method provides an operationally simple, robust and step-economical approach to the construction of diversely functionalized dihydroquinolinones bearing quaternary-centers. A sequential one-pot hydroalkylation-isomerization approach is also allowed giving access to a family of quinolinones. A wide substrate scope and high functional group tolerance was observed in both approaches</a>.

Diverse Cyclopentenes via Enantioselective Cu-Catalyzed Desymmetrization

2018 ◽  
Author(s):  
Reece Jacques ◽  
Robert D. C. Pullin ◽  
Stephen P. Fletcher
Keyword(s):  
Ring Systems ◽  
Quaternary Centers ◽  
Stereogenic Centers

<div> <div> <div> <p>A highly regio-, diastereo- and enantioselective Cu-catalyzed desymmetrization of diverse meso-bisphosphates with alkyl zirconium nucleophiles has been developed. The reaction allows access to a broad range of functionalized cyclopentenes with up to three contiguous stereogenic centers, including quaternary centers and spirocyclic ring systems.</p></div></div></div>

Diverse Cyclopentenes via Enantioselective Cu-Catalyzed Desymmetrization

2018 ◽  
Author(s):  
Reece Jacques ◽  
Robert D. C. Pullin ◽  
Stephen P. Fletcher
Keyword(s):  
Ring Systems ◽  
Quaternary Centers ◽  
Stereogenic Centers

<div> <div> <div> <p>A highly regio-, diastereo- and enantioselective Cu-catalyzed desymmetrization of diverse meso-bisphosphates with alkyl zirconium nucleophiles has been developed. The reaction allows access to a broad range of functionalized cyclopentenes with up to three contiguous stereogenic centers, including quaternary centers and spirocyclic ring systems.</p></div></div></div>

Synthesis of Nitrile-Bearing Quaternary Centers via an Equilibrium-Driven Transnitrilation and Anion-Relay Strategy

2019 ◽  
Author(s):  
Sebastien Alazet ◽  
Michael West ◽  
Purvish Patel ◽  
Sophie Rousseaux
Keyword(s):  
Building Blocks ◽  
One Pot ◽  
Quaternary Centers ◽  
Synthetic Intermediates

The efficient preparation of nitrile-containing building blocks is of interest due to their utility as synthetic intermediates and their prevalence in pharmaceuticals. As a result, significant efforts have been made to develop methods to access these motifs which rely on safer and non-toxic sources of CN. Herein, we report that 2-methyl-2-phenylpropanenitrile is an efficient, non-toxic, electrophilic CN source for the synthesis of nitrile-bearing quaternary centers via a thermodynamic transnitrilation and anion-relay strategy. This one-pot process leads to nitrile products resulting from the gem-difunctionalization of alkyl lithium reagents.<br>

Novel Piperazine Amides of Cinnamic Acid Derivatives as Tyrosinase Inhibitors

2018 ◽  
Vol 16 (1) ◽  
pp. 36-44 ◽  
Author(s):  
Zehra Tuğçe Gür ◽  
Fatma Sezer Şenol ◽  
Suhaib Shekfeh ◽  
İlkay Erdoğan Orhan ◽  
Erden Banoğlu ◽  
...  
Keyword(s):  
Cinnamic Acid ◽  
Active Site ◽  
Agaricus Bisporus ◽  
Biological Activities ◽  
Docking Simulation ◽  
Cinnamic Acid Derivatives ◽  
In Silico Docking ◽  
Amide Derivatives ◽  
Tyrosinase Inhibitors ◽  
Further Development

Background: A series of novel cinnamic acid piperazine amide derivatives has been designed and synthesized, and their biological activities were also evaluated as potential tyrosinase inhibitors. Methods: Compounds 9, 11 and 17 showed the most potent biological activity (IC50 = 66.5, 61.1 and 66 &#181;M, respectively). In silico docking simulation was performed to position compound 11 into the Agaricus bisporus mushroom tyrosinase’s active site to determine the putative binding interactions. Results and Conclusion: The results indicated that compound 11 could serve as a promising lead compound for further development of potent tyrosinase inhibitors.

Synthesis and Biological Activity of 28-Amide Derivatives of 23-Hydroxy Betulinic Acid as Antitumor Agent Candidates

2013 ◽  
Vol 9 (7) ◽  
pp. 920-925 ◽  
Author(s):  
Yi Bi ◽  
Jinyi Xu ◽  
Fei Sun ◽  
Xiaoming Wu ◽  
Wencai Ye ◽  
...  
Keyword(s):  
Biological Activity ◽  
Betulinic Acid ◽  
Antitumor Agent ◽  
Amide Derivatives ◽  
Derivatives Of
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