4 research outputs found
Multicomponent Assembly of Diverse Pyrazin-2(1<i>H</i>)‑one Chemotypes
An expedient and
concise Ugi-based approach for the rapid assembly
of pyrazin-2(1<i>H</i>)-one-based frameworks has been developed.
This convergent approach encompasses skeletal, functional and stereochemical
diversity, exhibiting an unusually high bond-forming efficiency as
well as high structure and step economies. The method involves the
use of readily available commercial reagents and is an example of
the reconciliation of structural complexity with operational simplicity
in a time- and cost-effective manner
Multicomponent Assembly of Diverse Pyrazin-2(1<i>H</i>)‑one Chemotypes
An expedient and
concise Ugi-based approach for the rapid assembly
of pyrazin-2(1<i>H</i>)-one-based frameworks has been developed.
This convergent approach encompasses skeletal, functional and stereochemical
diversity, exhibiting an unusually high bond-forming efficiency as
well as high structure and step economies. The method involves the
use of readily available commercial reagents and is an example of
the reconciliation of structural complexity with operational simplicity
in a time- and cost-effective manner
Copper-Catalyzed Huisgen 1,3-Dipolar Cycloaddition under Oxidative Conditions: Polymer-Assisted Assembly of 4‑Acyl-1-Substituted-1,2,3-Triazoles
We
herein document the first example of a reliable copper-catalyzed Huisgen
1,3-dipolar cycloaddition under oxidative conditions. The
combined use of two polymer-supported reagents (polystyrene-1,5,7-triazabicyclo[4,4,0]dec-5-ene/Cu
and polystyrene-2-iodoxybenzamide) overcomes the thermodynamic
instability of copper(I) species toward oxidation, enabling the reliable
Cu-catalyzed Huisgen
1,3-dipolar cycloadditions in the presence of an oxidant agent. This
polymer-assisted pathway, not feasible under conventional homogeneous
conditions, provides a direct assembly of 4-acyl-1-substituted-1,2,3-triazoles,
contributing to expand the reliability and scope of Cu(I)-catalyzed
alkyne–azide
cycloaddition
Discovery of 3,4-Dihydropyrimidin-2(1<i>H</i>)‑ones As a Novel Class of Potent and Selective A<sub>2B</sub> Adenosine Receptor Antagonists
We
describe the discovery and optimization of 3,4-dihydropyrimidin-2(1<i>H</i>)-ones as a novel family of (nonxanthine) A<sub>2B</sub> receptor antagonists that exhibit an unusually high selectivity
profile. The Biginelli-based hit optimization process enabled a thoughtful
exploration of the structure–activity and structure–selectivity
relationships for this chemotype, enabling the identification of ligands
that combine structural simplicity with excellent hA<sub>2B</sub> AdoR
affinity and remarkable selectivity profiles