Results 81 to 90 of about 5,649 (226)

Synthesis of aziridines and the functionalisation of the intact ring [PDF]

, 2015
Aziridines continue to offer synthetic interest, whilst providing important intermediates in the preparation of a variety of biologically active targets.
Boultwood, Tom
core   +1 more source

Copper(I)-catalyzed asymmetric decarboxylative Mannich reaction enabled by acidic activation of 2H-azirines

Nature Communications, 2019
Due to their poor electrophilicity, 2H-azirines do not easily react with nucleophiles. Here, the authors show an acidic activation of 2H-azirines by cyanoacetic acid coupling partners affording chiral aziridines containing vicinal tetrasubstituted and ...
Hai-Jun Zhang, Yan-Cheng Xie, Liang Yin
doaj   +1 more source

Selective Rh(II)‐Catalyzed Intermolecular Oxyamidation and Acid‐Promoted Nucleophilic Cyclization Cascade of Enamides

ChemistryEurope, Volume 4, Issue 6, June 2026.
A structurally diverse series of 1‐amino‐izidine scaffolds was accessed through a cascade process combining rhodium‐catalyzed nitrene‐transfer oxyamidation with subsequent nucleophilic cyclization under acidic conditions, proceeding via an in situ generated iminium intermediate.
Grégory Jestin, Romain Rey‐Rodriguez, Romane Manguin, Pascal Retailleau, Philippe Dauban, Isabelle Gillaizeau   +5 more
wiley   +1 more source

The asymmetric synthesis of aziridines

, 1997
The report contains an overview of methods available for asymmetric preparation of a range of 1H- aziridines and their N-substituted ...
Sweeney, Joseph B., Osborn, Helen M.I.
core   +1 more source

Single‐Sequence Deep Learning Delivers Crystal‐Quality Models of Covalent K‐Ras G12 Hotspot Complexes

IUBMB Life, Volume 78, Issue 6, June 2026.
ABSTRACT Structure‐based design of covalent drugs has achieved tremendous success by understanding and leveraging the three‐dimensional interactions between small‐molecule drug candidates and their protein targets. However, this approach traditionally relies on high‐resolution co‐complex structures obtained by X‐ray crystallography, NMR, or cryo‐EM ...
Sungwon Jung, Qinheng Zheng, Kevan M. Shokat   +2 more
wiley   +1 more source

Highly Efficient Asymmetric [3+2] Cycloaddition Promoted by Chiral Aziridine-Functionalized Organophosphorus Compounds

Molecules
The asymmetric [3+2] cycloaddition of azomethine ylides generated from the corresponding imino ester-to-trans-β-nitrostyrene catalysis by chiral aziridine-containing phosphines and phosphine oxides is described. Of the sixteen stereoisomers that could be
Julia Szymańska, Michał Rachwalski, Adam M. Pieczonka   +2 more
doaj   +1 more source

Unexpected ring-opening reactions of aziridines with aldehydes catalyzed by nucleophilic carbenes under aerobic conditions

, 2006
The chemoselective ring opening of N-tosyl aziridines with aldehydes catalyzed by an N-heterocyclic carbene was investigated under aerobic conditions. Unexpected carboxylates of 1,2-amino alcohols from the corresponding aldehydes, rather than the acyl ...
Yue, L, Liu, YK, Li, BJ, Liu, YK, Sichuan Univ, W China Sch Pharm, Educ Minist, Key LDrug Targeting, Chengdu 610041, Peoples R China., Wu, Y, Ding, LS, Li, R, Chen, YC   +7 more
core  

Synthesis of N–H Aziridines from Unactivated Olefins Using Hydroxylamine-O-Sulfonic Acids as Aminating Agent

Herein, we presented a practical methodology for the intermolecular aziridination of alkenes, using HOSA as the aminating agent, alongside pyridine or piperidine as the base, within HFIP solvent system.
Gang, He, Gong, Chen, Yi, Huang, Shiyang, Zhu, Hao, Wang   +4 more
core   +1 more source

The synthesis and reactivity of n-diphenylphosphinyl aziridines

, 1994
The synthesis of enantiopure N-diphenylphosphinyl (Dpp) protected aziridines from 2-aminoalcohols and the reactions of these aziridines with a range of nucleophiles is ...
Howson, Bill, Sweeney, J. B., Sweeney, Joseph B., Osborn, Helen, Osborn, Helen M.I., Sweeney, JB, Osborn, HMI, Howson, B   +7 more
core   +1 more source

Recent Advances in Intramolecular C─N Bond Formation for Pyrrolidine Synthesis

ChemistryOpen, Volume 15, Issue 6, June 2026.
This review highlights synthetic advances (2013–2025) in intramolecular C─N bond formation for constructing the pharmaceutically relevant pyrrolidine core. The review is organized into five methodological clusters: 1) intramolecular alkene/alkyne amination; 2) tandem annulations, which involve C─N bond formation as the key step; 3) nucleophilic ...
Rasma Kroņkalne, Māris Turks
wiley   +1 more source