ChemInform Abstract: C-H Functionalization of Terminal Alkynes Towards Stereospecific Synthesis of (E) or (Z) 2-Methylthio-1,4-ene-diones.

ChemInform ◽  
2015 ◽  
Vol 46 (30) ◽  
pp. no-no
Author(s):  
Shekaraiah Devari ◽  
Arvind Kumar ◽  
Ramesh Deshidi ◽  
Bhahwal Ali Shah
Keyword(s):  
Stereospecific Synthesis ◽  
Terminal Alkynes

C–H functionalization of terminal alkynes towards stereospecific synthesis of (E) or (Z) 2-methylthio-1,4-ene-diones

2015 ◽  
Vol 51 (24) ◽  
pp. 5013-5016 ◽  
Author(s):  
Shekaraiah Devari ◽  
Arvind Kumar ◽  
Ramesh Deshidi ◽  
Bhahwal Ali Shah
Keyword(s):  
Stereospecific Synthesis ◽  
Terminal Alkynes ◽  
Metal Free

An efficient metal free self-sorting tandem protocol for stereospecific synthesis of (E) or (Z) 2-methylthio-1,4-ene-diones has been developed.

Synthesis of Novel 1,2,3-Triazole Derivatives of Isocoumarins and 3,4-Dihydroisocoumarin with Potential Antiplasmodial Activity In Vitro

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 ◽  
...  
Keyword(s):  
Triazole Ring ◽  
Antiplasmodial Activity ◽  
World Health ◽  
Dipolar Cycloaddition ◽  
Terminal Alkynes ◽  
The World ◽  
Ic50 Values ◽  
Derivatives Of ◽  
Active Substances

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.

Stereospecific Synthesis of m-Hydroxymexiletine Enantiomers

2013 ◽  
Vol 6 (3) ◽  
pp. 182-186 ◽  
Author(s):  
Alessia Catalano ◽  
Alessia Carocci ◽  
Giovanni Lentini ◽  
Ivana Defrenza ◽  
Claudio Bruno ◽  
...  
Keyword(s):  
Stereospecific Synthesis
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