Reductive amination plays a key role in the medicinal chemistry toolbox since it allows the mono alkylation of an amine or aniline. In this work, reductive amination of functionalized aldehydes with aniline derivatives of adenine and closely related 7-deazapurines has been successfully performed using H-cube technology so that imine formation and its reduction are performed "". The set-up procedure surmounts some of the drawbacks of "in batch" protocols by avoiding the handling of reductant reagents, long reaction times and tedious work-ups. The here described procedure allows a high conversion into the reductive amination products together with an easy work-up by just evaporation. More interestingly, this set-up does not require the presence of acids so that acid-sensitive protecting groups can be present both at the aldehyde and at the heterocycle.
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http://dx.doi.org/10.1039/d3ob00822c | DOI Listing |
Org Lett
January 2025
School of Chemistry and Chemical Engineering, Nanchang University, Nanchang, Jiangxi 330031, P. R. China.
A Ni/photoredox dual-catalyzed multicomponent cross-electrophile coupling of N-vinyl amides with (hetero)aryl halides and (2°, 3°)-alkyl redox-active esters in the presence of cheap reductant Hantzsch ester is reported here. This reductive protocol provides direct access to various synthetically challenging chiral α-arylamides in good yields and excellent enantioselectivities (up to 99% ee, with the majority exceeding 97% ee), which can be further derived into chiral primary and secondary amines. Preliminary experimental studies shed light on the potential catalytic pathways.
View Article and Find Full Text PDFMol Biol Rep
January 2025
Biochemistry Department, Faculty of Science, Ain Shams University, Cairo, Egypt.
Background: Exposure to ionizing radiation is inevitable due to its extensive use in industrial and medical applications. The search for effective and safe natural therapeutic agents as alternatives to chemical drugs is crucial to mitigate their side effects. This study aimed to evaluate the effects of citicoline as a standalone treatment or in combination with the anti-hepatotoxic drug silymarin in protecting against liver injury caused by γ-radiation in rats.
View Article and Find Full Text PDFACS Appl Mater Interfaces
January 2025
Key Laboratory of Green Chemistry & Technology, Ministry of Education, College of Chemistry, Sichuan University, Chengdu, Sichuan 610064, P.R. China.
Primary diamines are valuable yet challenging to synthesize due to issues such as product and intermediate condensation and catalyst poisoning. To address these problems, effective synthesis systems must be explored. Here, 2,5-bis(aminomethyl)furan (BAMF), a biomass-derived primary diamine, is chosen as the model for constructing such a system.
View Article and Find Full Text PDFOrg Lett
January 2025
School of Environmental and Chemical Engineering, Wuyi University, Jiangmen 529090, P. R. China.
We have realized a cathodic deoxygenative alkylation between nitro(hetero)arenes and organic halides, employing bis(pinacolato)diboron (Bpin) and LiCl as additives to trap and stabilize the generated alkyl radicals and carbanions, thereby facilitating efficient N-O cleavage and selective C-N bond formation. The protocol offers an economical method for the efficient synthesis of multiple aromatic(hetero) amines, without the need for reactive reductants and the exclusion of air and moisture. Notably, the protocol is distinguished by scalability, broad functional group compatibility, and safe and mild conditions, demonstrating practicality in the synthesis and late-stage modification of various bioactive compounds.
View Article and Find Full Text PDFInt J Nanomedicine
January 2025
Advanced Diagnostics and Therapeutics Institute, Health Sector, King Abdulaziz City for Science and Technology (KACST), Riyadh, 11442, Saudi Arabia.
Introduction: Wound treatment is a significant health burden in any healthcare system, which requires proper management to minimize pain and prevent bacterial infections that can complicate the wound healing process.
Rationale: There is a need to develop innovative therapies to accelerate wound healing cost-effectively. Herein, two polymer-based nanofibrous systems were developed using poly-lactic-co-glycolic-acid (PLGA) and polyvinylpyrrolidone (PVP) loaded with a combination of an antibiotic (Fusidic acid, FA) and a local anesthetic (Lidocaine, LDC) via electrospinning technique for an expedited healing process by preventing bacterial infections while reducing the pain sensation.
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