Publication of the Week

Efficient Synthesis of Chiral ProTides through Copper Catalysis
Efficient Synthesis of Chiral ProTides through Copper Catalysis

A new study introduces a novel method for the stereoselective synthesis of chiral phosphates in ProTide nucleoside analogues.

Nov 13, 2024

Exploring Anti-Bredt Olefins as Reactive Intermediates
Exploring Anti-Bredt Olefins as Reactive Intermediates

The access and the usage of anti-Bredt type olefins as intermediates are described in a new study in Science.

Nov 10, 2024

Macrocycles can lock the Conformation of Drug Candidates and enhance their Activity
Macrocycles can lock the Conformation of Drug Candidates and enhance their Activity

Macrocycles can improve the conformation, biological activity, selectivity, ADME properties, and target affinity of small-molecule drug candidates.

Sep 10, 2024

Synthesis of Quaternary Centres using Lithium Enolates in a Ru-catalysed Allylic substitution
Synthesis of Quaternary Centres using Lithium Enolates in a Ru-catalysed Allylic substitution

The construction of quaternary centers via C-C bond formation is a significant challenge, but a new method reported in JACS, provides a promising approach to accessing these sterically crowded motifs.

Aug 24, 2024

Synthesis of Drug Libraries using Sulfamide Linker Strategy
Synthesis of Drug Libraries using Sulfamide Linker Strategy

A coupling strategy ready for use in a 96 well plate.

Aug 21, 2024

Ring Closing Alkyne Metathesis allows unified Synthesis of Strasseriolides A to D
Ring Closing Alkyne Metathesis allows unified Synthesis of Strasseriolides A to D

Synthesis of stasseriolide natural products and their analogues using a ring-closing alkyne metathesis by Alois Fürstner and his team.

Aug 10, 2024

Pfizer's Second-Generation SARS-CoV-2 Protease Inhibitor
Pfizer's Second-Generation SARS-CoV-2 Protease Inhibitor

Researchers from Pfizer have developed a structurally-optimized SARS-CoV-2 main protease inhibitor with improved metabolic stability compared to nirmatrelvir which is now in clinical trials.

Jul 27, 2024

Biocatalytic diversification of thionucleoside analogues
Biocatalytic diversification of thionucleoside analogues

Novel biocatalytic method for the diversification of thionucleosides, demonstrating that enzyme-catalyzed transglycosylation can effectively facilitate nucleobase exchange.

Jul 23, 2024

Breaking the aromaticity of thiophene using a [4+3] cycloaddition
Breaking the aromaticity of thiophene using a [4+3] cycloaddition

A novel dearomative, intramolecular [4+3]-cycloaddition of thiophenes at low temperatures yielding complex tricyclic ring systems.

Jul 19, 2024

Novel remdesivir type nucleoside analogue displays broad-spectrum antiviral activity
Novel remdesivir type nucleoside analogue displays broad-spectrum antiviral activity

The development of a novel 4'-CN remdesivir-type nucleoside analogue demonstrating the potential of 4-aza-7,9-dideazaadenosine nucleoside analogues to exhibit antiviral activity.

Jul 15, 2024