The synthesis of 1 beta-methylcarbapenems having a ROCH2 substituent at the 2-position is described. Their in vitro antibacterial activity and DHP-I susceptibilities are presented.
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One Step Synthesis of 4,6,8-Trimethoxyazulenes - as Building Block for 2-Functionalized Azulenes.
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Organisch-Chemisches Institut, Heidelberg University, Im Neuenheimer Feld 270, 69120, Heidelberg, Germany.
Here we present a simple gold-catalyzed one-pot reaction of easily available diarylbutadiynes, with trimethoxybenzene as solvent and reactant to synthesize 4,6,8-trimethoxyazulenes. The methoxy substituents, which render the azulene very electron-rich, enable a change of azulenes typical regioselectivity for electrophilic substitutions, which enables facile electrophilic 2-substitution with iodine, bromine, chlorine, selenium or sulfur. Especially the 2-haloazulenes which can usually only be obtained through lengthy multistep syntheses are valuable building blocks for the synthesis of 2-substituted azulene derivatives.
View Article and Find Full Text PDFDirect Synthesis of 2-Functionalized 3-Nitroindoles from Diazo(nitro)acetanilides.
J Org Chem
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State Key Laboratory of Chemical Resource Engineering, Department of Organic Chemistry, College of Chemistry, Beijing University of Chemical Technology, Beijing 100029, People's Republic of China.
2-Hydroxyl/acetoxy-3-nitroindoles are directly and efficiently prepared in good to excellent yields from diazo(nitro)acetanilides under the catalysis of Cu(MeCN)PF in DCM through an intramolecular aromatic C-H insertion or followed by acetylation. 2-Hydroxyl-3-nitroindoles can be further transformed to 3-halo-3-nitroindolin-2-ones and 3-alkanamidoindolin-2-ones readily. All of them are important synthetic building blocks for construction of indole derivatives.
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Gold nanoparticles (AuNPs) present with unique physicochemical features and potential for functionalization as anticancer agents. Three-dimensional spheroid models can be used to afford greater tissue representation due to their heterogeneous phenotype and complex molecular architecture. This study developed an A549 alveolar carcinoma spheroid model for cytotoxicity assessment and mechanistic evaluation of functionalized AuNPs.
View Article and Find Full Text PDFDesign, Synthesis, and Antibacterial Activities of Multi-Functional C-Functionalized 1,4-Naphthoquinonyl Organoseleniums.
Chem Asian J
December 2024
Department of Chemistry, Indian Institute of Science Education and Research Bhopal, Bhopal By-pass Road, Bhauri, Bhopal, Madhya Pradesh 462066, India.
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View Article and Find Full Text PDFSynthesis of 2-Amino-quinazolin-4()-ones Using 2-Bromo--phenylbenzamide and Cyanamide Ullmann Cross-Coupling.
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State Key Laboratory of High-efficiency Utilization of Coal and Green Chemical Engineering, College of Chemistry and Chemical Engineering, Ningxia University, Yinchuan 750001, China.
Article Synopsis
- A new method was developed to create 2-amino-3-substituted quinoline-4(3)-ones and -phenylbenzamide derivatives using inexpensive materials and a simple process.
- The synthesis involves Ullmann cross-coupling with cyanamide, 2-bromo-phenylbenzamide, copper iodide, and potassium tert-butoxide in dimethyl sulfoxide, all of which can be done under air conditions without ligands.
- Additionally, the research shows that other nucleophilic reagents like water and amines can also be used to produce 2-functionalized phenylbenzamides.
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