Synthesis and in Silico Study of Novel Benzisoxazole‐Chromene Derivatives as Potent Inhibitors of Acetylcholinesterase: Metal‐Free Site‐Selective C−N Bond Formation via Aza‐Michael Reaction DOI
Grace Victoria Govada, Sabbasani Rajasekhara Reddy

Chemistry & Biodiversity, Journal Year: 2023, Volume and Issue: 20(8)

Published: July 7, 2023

Abstract An efficient metal‐free approach for site selective C−N coupling reaction of benzo[d]isoxazole and 2 H ‐chromene derivatives has been designed developed against AchE. This nitrogen containing organo‐base promoted methodology, which is both practical environmentally friendly, provides an easy suitable pathway synthesizing Benzisoxazole‐Chromene (BC) possessing poly heteroaryl moieties. The synthesized BC 4 a – n was docked into the active sites AChE to obtain more perception binding modes compounds. Out them, compound l displayed potent activity high selectivity inhibition. Final docking results indicates that showed lowest energy −11.2260 kcal/mol with AChE. analogs would be potential candidates promoting studies in medicinal chemistry research.

Language: Английский

Visible-light-mediated C(sp3)–H functionalization of alkyl arylacetates: an easy approach to S-benzyl dithiocarbamate acetates DOI

Mahesh Kumar,

Ramesh Kumar Vishwakarma,

Preeti Preeti

et al.

New Journal of Chemistry, Journal Year: 2022, Volume and Issue: 47(5), P. 2412 - 2416

Published: Dec. 22, 2022

An efficient visible light-promoted C(sp 3 )–H functionalization of alkyl arylacetates has been developed using CS 2 and amines by eosin Y/I dual catalysis to achieve the formation S -benzyl dithiocarbamate acetates.

Language: Английский

Citations

3
1,6-Nucleophilic Di- and Trifluoromethylation of para-Quinone Methides with Me3SiCF2H/Me3SiCF3 Facilitated by CsF/18-Crown-6 DOI Creative Commons
Dingben Chen, Ling Huang,

Mingyu Liang

et al.

Molecules, Journal Year: 2024, Volume and Issue: 29(12), P. 2905 - 2905

Published: June 19, 2024

The direct 1,6-nucleophilic difluoromethylation, trifluoromethylation, and difluoroalkylation of para-quinone methides (p-QMs) with Me3SiRf (Rf = CF2H, CF3, CF2CF3, CF2COOEt, CF2SPh) under mild conditions are described. Although Me3SiCF2H shows lower reactivity than Me3SiCF3, it can react p-QMs promoted by CsF/18-Crown-6 to give structurally diverse difluoromethyl products in good yields. then be further converted into fluoroalkylated α-fluoroalkylated diarylmethanes.

Language: Английский

Citations

0
Pd(II)‐Catalyzed Site‐Selective Cross Coupling Reaction: Synthesis of Highly Fluorescent Aryl−Formyl−Chromenes and its Iminoantipyrine Analogues as Selective AChE Inhibitors DOI
Grace Victoria Govada,

Sanjivani Pal,

Paranimuthu Panjacharam

et al.

Chemistry & Biodiversity, Journal Year: 2024, Volume and Issue: 21(8)

Published: July 3, 2024

A versatile and efficient chemo selective synthesis of 4-aryl-3-formyl-2H-chromenes (AFC) was undertaken using Pd-catalyzed cross-coupling conditions. The key oxidative transmetalation successfully applied to a significant range substitutions on the chromene moiety aryl ring in Ar(BOH)

Language: Английский

Citations

0
Synthesis of N-benzyl pyridones from para-quinone methides (p-QMs) at room temperature: Evaluation of in vitro blood-stage antiplasmodial activity DOI
Rapelly Venkatesh,

Keerthana Gurukkalot,

Vinoth Rajendran

et al.

Organic & Biomolecular Chemistry, Journal Year: 2024, Volume and Issue: unknown

Published: Jan. 1, 2024

Synthesis of N -benzyl pyridones from para -quinone methides ( p -QMs) and 2- or 4-hydroxy pyridines is presented. The synthesized displayed significant in vitro blood-stage antiplasmodial activity.

Language: Английский

Citations

0
Synthesis and in Silico Study of Novel Benzisoxazole‐Chromene Derivatives as Potent Inhibitors of Acetylcholinesterase: Metal‐Free Site‐Selective C−N Bond Formation via Aza‐Michael Reaction DOI
Grace Victoria Govada, Sabbasani Rajasekhara Reddy

Chemistry & Biodiversity, Journal Year: 2023, Volume and Issue: 20(8)

Published: July 7, 2023

Abstract An efficient metal‐free approach for site selective C−N coupling reaction of benzo[d]isoxazole and 2 H ‐chromene derivatives has been designed developed against AchE. This nitrogen containing organo‐base promoted methodology, which is both practical environmentally friendly, provides an easy suitable pathway synthesizing Benzisoxazole‐Chromene (BC) possessing poly heteroaryl moieties. The synthesized BC 4 a – n was docked into the active sites AChE to obtain more perception binding modes compounds. Out them, compound l displayed potent activity high selectivity inhibition. Final docking results indicates that showed lowest energy −11.2260 kcal/mol with AChE. analogs would be potential candidates promoting studies in medicinal chemistry research.

Language: Английский

Citations

1