Results 61 to 70 of about 7,765 (231)
Small ring heterocycles, such as epoxides and aziridines, are present in several natural products and are also highly versatile building blocks, frequently involved in the synthesis of numerous bioactive products and pharmaceuticals.
Allan Ribeiro da Silva +3 more
doaj +1 more source
Covalent drug discovery: Progress against key targets, emerging strategies and lessons learnt
Abstract Covalent drug discovery is currently experiencing a boom in industrial and academic interest. To date, at least 75 covalent drugs have received regulatory approval, targeting both traditional target classes and more challenging proteins for which other approaches failed. In many cases, unique aspects of covalent targeting are essential for the
Charles P. Brown +2 more
wiley +1 more source
The transition from linear to cyclic organic cations promotes deprotonation and activates VH(N) defects with pronounced lone‐pair electron activity, thereby inducing severe local distortions and highly efficient nonradiative recombination centers. This work unveils a direct structure–defect–performance correlation and proposes design strategies for the
Qingshan Bao +5 more
wiley +1 more source
Aziridine-2-carboxylic acid derivatives and its open-ring isomers as a novel PDIA1 inhibitors
Acyl derivatives of aziridine-2-carboxylic acid have been synthesized and tested as PDIA1 inhibitors. Calculations of charge value and distribution in aziridine ring system and some alkylating agents were performed. For the first time was found that acyl
Kalvins, Ivars +8 more
core +1 more source
Recent Studies of (+)-3-Carene Transformations with the Retention of the Native Framework
This review presents last decade and some past especially relevant studies in the field of (+)-3-carene synthetic transformations. This paper discusses exclusively the transformations of (+)-3-carene, proceeding with the retention of the native bicyclic ...
Serghei Curlat
doaj +1 more source
A modular Rh‐catalyzed synthetic approach enabled the preparation of diverse reactive fragments from available substrates. The reactive fragments modified Aurora A kinase via several distinct modification reaction classes. In a complex biological environment, the constellation of modified proteins depended critically on the reactive fragment structure.
Julian Chesti +8 more
wiley +1 more source
Cis-2-iminothiazolidines and cis-thiazolidine-2-iminium tetrafluoroborates were successfully produced from trans-N-alkyl aziridine-2-carboxylates and phenyl/alkyl isothiocyanates mediated by zinc tetrafluoroborate in refluxing DCE.
Chayma Ben Maamer (11261033) +9 more
core +2 more sources
Aziridinierung eines einzelnen Kohlenstoffatoms in Alkenen mittels Energietransferkatalyse
Im Gegensatz zur traditionellen Alken‐Aziridinierung über (formalen) Nitren‐Transfer berichten wir hier über eine Strategie zur intermolekularen Aziridinierung eines einzelnen Alken‐Kohlenstoffatoms bei zusätzlicher Funktionalisierung der anderen Position. Durch Energietransfer‐ (EnT‐)Katalyse werden Alkenylboronate und ‐silane in reaktive Intermediate
Fritz Paulus +7 more
wiley +1 more source
Asymmetric Syntheses of Aziridine-2-carboxylates via Reductive Kinetic Resolution of 2H-Azirines
Enantioenriched aziridine-2-carboxylates are valuable organic compounds thanks to their versatility as chiral building blocks. Several syntheses of bioactive molecules employ aziridine-2-carboxylates as a crucial synthetic intermediate, e.g.
Antonio, Rizzo +2 more
core +1 more source
1,1‐Disubstituted vinylbromides are key intermediates for constructing nitrogen‐containing heterocycles. This review provides an overview of the synthetic applications of 1,1‐disubstituted vinylbromides and summarizes recent developments in reaction methodologies, mechanistic insights, and the structural diversity of N‐heterocyclic compounds accessible
Anne Westermeyer +6 more
wiley +1 more source

