Anticancer evaluations of iodoquinazoline substituted with allyl and/or benzyl as dual inhibitors of EGFR^WT and EGFR^T790M: design, synthesis, ADMET and molecular docking

RSC Advances, Journal Year: 2024, Volume and Issue: 14(12), P. 7964 - 7980

Published: Jan. 1, 2024

Fifteen new iodoquinazoline derivatives, 5a,b to 18, are reported in this study and their anticancer evaluation as dual inhibitors of EGFR WT T790M .

Language: Английский

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Efficient and Sustainable Electrosynthesis of N-Sulfonyl Iminophosphoranes by the Dehydrogenative P–N Coupling Reaction

JACS Au, Journal Year: 2024, Volume and Issue: 4(6), P. 2188 - 2196

Published: April 18, 2024

Iminophosphoranes are commonly used reagents in organic synthesis and are, therefore, of great interest. An efficient sustainable iodide-mediated electrochemical N-sulfonyl iminophosphoranes from readily available phosphines sulfonamides is reported. This method features low amounts supporting electrolytes, inexpensive electrode materials, a simple galvanostatic setup, high conversion rates. The broad applicability could be demonstrated by synthesizing 20 examples yields up to 90%, having diverse functional groups including chiral moieties biologically relevant species. Furthermore, electrolysis was performed on g scale run repetitive mode recycling the electrolyte, which illustrates suitability for large-scale production. A reaction mechanism involving mediation iodide-based electrolyte proposed, completely agreeing with all results.

Language: Английский

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Facile Synthesis of 2-Substituted Quinazolines via Ruthenium(II)-Catalyzed Acceptorless Dehydrogenative Coupling

Current Organic Chemistry, Journal Year: 2024, Volume and Issue: 28(4), P. 305 - 318

Published: Feb. 1, 2024

Abstract:: This study aims to develop a practical and facile one-pot synthesis of 2- substituted quinazolines. Using commercially available structurally simple ruthenium( II) complex as the catalyst synthesize series quinazoline derivatives via acceptorless dehydrogenative coupling. The mechanism this reaction was explored by control DFT calculation. protocol offers access diverse array (52 examples) in moderate excellent yields (29%-98%). In summary, we have developed an efficient ruthenium (II)-catalyzed ADC under air atmosphere. only produces hydrogen water by-products, serving sustainable atom-efficient synthetic approach.

Language: Английский

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Azidoindolines—From Synthesis to Application: A Review

Chemistry, Journal Year: 2024, Volume and Issue: 6(4), P. 556 - 580

Published: July 18, 2024

Azide-containing compounds, organic azides, showcases a variety of reactivities, making them highly convenient and chameleonic intermediates. An indoline derivative has been proven to be great significance in drug discovery due its sp3-rich property. In this context, it is interesting perform such vigorous azidation on medicinal-relevant indoles/indolines, resulting the production azidoindolines. The potential biological activity, combination with bearing azido moiety, makes azidoindolines an attractive synthetic target for medicinal chemists. This review describes recent advances synthesis application azidoindolines: (1) iodine-mediated azidations, (2) metal-catalyzed (3) electrochemical (4) photochemical (5) using oxidant azide source, (6) nucleophilic azidation.

Language: Английский

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