Photochemical thiocarbonyl difluoride generation enables azetidine synthesis [PDF]
The activation of amines into thiocarbamoyl fluorides (TCarbFs) provides access to valuable nitrogen-based functionalities. However, their broader use has been hindered by the reliance on harsh reagents and conditions.
Ricardo I. Rodríguez +9 more
doaj +4 more sources
Rare Gold-Catalyzed 4-exo-dig Cyclization for Ring Expansion of Propargylic Aziridines toward Stereoselective (Z)-Alkylidene Azetidines, via Diborylalkyl Homopropargyl Amines. [PDF]
We report an uncommon 4-exo-dig cyclization of N-tosyl homopropargyl amines, catalyzed by [AuCl(PEt3)]/AgOTf, to prepare stereoselective (Z)-2-alkylidene-1-tosylazetidine compounds.
Salvadó O +5 more
europepmc +4 more sources
Palladium and Platinum 2,4-cis-amino Azetidine and Related Complexes [PDF]
Seven N,N'-palladium(II) chloride complexes, one N,N'-palladium(II) acetate complex of 2,4-cis-azetidines where prepared and analyzed by single crystal XRD.
Akina Yoshizawa +4 more
doaj +6 more sources
Studies on the interaction of isocyanides with imines: reaction scope and mechanistic variations [PDF]
The interaction of imines with isocyanides has been studied. The main product results from a sequential process involving the attack of two units of isocyanide, under Lewis acid catalysis, upon the carbon–nitrogen double bond of the imine to form the 4 ...
Ouldouz Ghashghaei +4 more
doaj +2 more sources
HFIP-assisted Brønsted acid-catalyzed ring opening of 1-azabicyclo[1.1.0]butane to access diverse C3-quaternary aza-azetidines and indole-azetidines [PDF]
Nitrogen-based heterocycles represent 60% of small-molecule-approved drugs. Increasing demand for sp3-rich N-heterocyclic scaffolds as a bioisosteric replacement in drug discovery platforms has continued to drive the development of elegant methods for ...
Subrata Hazra +6 more
doaj +2 more sources
Azetidine synthesis enabled by photo-induced copper catalysis via [3+1] radical cascade cyclization
Azetidines are an important type of saturated, highly strained, four-membered, nitrogen-containing heterocyclic compound. These compounds serve as important raw materials, intermediates, and catalysts in organic synthesis, as well as important active ...
Jianye Li +8 more
doaj +2 more sources
Structural basis of malaria parasite phenylalanine tRNA-synthetase inhibition by bicyclic azetidines [PDF]
Bicyclic azetidine inhibitors are promising antimalarials that target the Plasmodium cytosolic phenylalanine tRNAsynthetase (cFRS). Here, Sharma et al.
Manmohan Sharma +11 more
doaj +2 more sources
Rigid and concave, 2,4-cis-substituted azetidine derivatives: A platform for asymmetric catalysis. [PDF]
A series of single enantiomer, 2,4-cis-disubstituted amino azetidines were synthesised and used as ligands for copper-catalysed Henry reactions of aldehydes with nitromethane. Optimisation of ligand substituents and the reaction conditions was conducted.
Feula, A +4 more
core +6 more sources
Bicyclic azetidines target acute and chronic stages of Toxoplasma gondii by inhibiting parasite phenylalanyl t-RNA synthetase [PDF]
Current treatments for toxoplasmosis are limited by adverse reactions and inability to cure chronic infections dominated by semi-dormant cyst forms. Here the authors demonstrate the potential of small molecule inhibitors of PheRS for controlling acute ...
Joshua B. Radke +12 more
doaj +2 more sources
Asymmetric synthesis of α,β-diamino acid derivatives with an aziridine-, azetidine- and γ-lactone-skeleton via Mannich-type additions across α-chloro- N-sulfinylimines [PDF]
The efficient asymmetric synthesis of new chiral γ-chloro-α,β-diamino acid derivatives via highly diastereoselective Mannich-type reactions of N-(diphenylmethylene) glycine esters across a chiral α-chloro-N-p-toluenesulfinylimine was developed.
Callebaut, Gert +5 more
core +4 more sources

