Events & News

Events & News

Optimizing Hydroxyl Groups: The Tertiary Alcohol Advantage in Medicinal Chemistry

Previous research has established that the strategic substitution of a hydrogen atom with a hydroxyl group (H-to-OH) effectively diminishes molecular lipophilicity, enhances aqueous solubility, and attenuates hERG inhibition. Notwithstanding these advantageous properties, hydroxyl groups (OH) are not universally preferred in pharmaceutical design. This selectivity arises because in primary and secondary alcohols, the OH moiety constitutes a metabolic vulnerability, susceptible to oxidative processes and glucuronidation reactions. Furthermore, hydroxyl groups may adversely affect cell membrane permeability parameters. Conversely, tertiary alcohols (3° ROH) frequently demonstrate superior metabolic profiles. This enhancement stems from the structural configuration of 3° ROH, where oxidation at the carbon-hydroxyl junction is sterically hindered, and adjacent alkyl substituents provide protective steric effects to the OH group, thereby reducing susceptibility to glucuronidation and mitigating permeability constraints.

2025-07-15

Modular Arene Functionalization by Differential 1,2-Diborylation

A nickel-catalyzed vicinal diborylation method that 12 can directly install two chemically differentiated boryl groups in a regio- and site-selective manner using readily 13 available aryl triflates or chlorides as substrates. This reaction operates under mild reaction conditions and shows a broad substrate scope and excellent functional group tolerance. Each boryl group can be independently transformed into various groups, providing an efficient modular, regioselective, and divergent approach to access diverse vicinal difunctionalized arenes, showing promise for constructing analogue libraries.

2025-07-14

Copper-Catalyzed Enantioselective Three-Component Carboamidation of Styrenes with Alkanes and Amides

The efficient assembly of valuable chiral molecules from readily available and low-cost chemical feedstocks remains one of the most challenging tasks in synthetic chemistry today. Radical-mediated three-component carboamination of alkenes offers an attractive strategy for addressing this challenge. However, most existing reports focus on racemic examples and are largely limited to activated alkenes, preactivated alkylation reagents, or sufficiently active nucleophiles. Herein, the authors report a highly enantioselective three-component carboamidation of styrenes with unactivated alkanes and weakly nucleophilic amides. Enantioselective control is achieved by using chiral cationic copper catalysts. This method enables the synthesis of various optically active amides with excellent enantioselectivity. Mechanistic studies reveal that the reaction proceeds via hydrogen atom transfer from the alkane, followed by radical addition to the olefin.

2025-07-09

Novel Difluorocyclobutyl Derivatives as Potent Glucagon-Like Peptide-1 Receptor Agonists with Reduced hERG Inhibitory Activity

Research conducted at the College of Ocean, Zhejiang University, by Professor Wanjing Ding and Professor Zhongjun Ma has led to significant advances in pharmaceutical development.

2025-06-17

STAT3: A Critical Target in Cancer Research

In the frontier of cancer research, STAT3 emerges as a crucial signalling molecule expressed across various tissues, regulating genes associated with cancer cell growth, proliferation, angiogenesis, metastasis, drug resistance, and immune evasion. Its persistent activation is implicated in multiple oncogenic mechanisms, establishing it as a primary target in cancer research.

2025-05-29

Advances in the Synthesis of Cyclopropylamine

Professor Philippe Bertus , currently affiliated with the Centre National de la Recherche Scientifique (CNRS) and Le Mans Université , spent years specializing in organic and polymer chemistry. His research portfolio comprises over 110 scientific publications encompassing organic synthesis and catalytic reactions. In collaboration with Julien Caillé, they contributed a comprehensive review titled "Advances in the Synthesis of Cyclopropylamines" that outlines recent methodological breakthroughs in the field.

2025-05-16

From Mechanism to Medicine: Recent Advances in Ferroptosis from Top-Tier Publications

Ferroptosis is a distinct form of programmed cell death characterized by iron-dependent lipid peroxidation, first formally described by Dr.Brent Stockwell in 2012. Unlike apoptosis, necrosis, and autophagy, ferroptosis is driven by intracellular iron accumulation and lipid peroxides.

2025-04-30

Sulfilimines: An Underexplored Bioisostere for Drug Design?

In the ever-evolving landscape of medicinal chemistry, searching for novel functional groups with optimized pharmacological properties remains a key driver of innovation. While sulfoximines have gained increasing traction as aza-analogs of sulfones in both FDA-approved drugs and agrochemicals, a newer class—sulfilimines—is now emerging as a promising, underutilized scaffold for drug design. Pioneering studies by Ellman, Gnamm, and most recently by Arvidsson and Ritter’s groups have demonstrated the chemical versatility, metabolic stability, and synthetic utility of sulfilimines in the development of bioactive molecules.

2025-04-21

World Cancer Day 2025: Breakthroughs and Trends in Anti-Cancer Drug Development

On World Cancer Day 2025, we reflect on the progress in cancer research, especially small-molecule drugs and precision medicine. Advances in AI and targeted therapies are transforming cancer care, and AmBeed proudly supports researchers driving these breakthroughs. Together, we move closer to a cancer-free future.

2025-02-04

Harnessing Photocatalytic Single-Electron Oxidation: Radical Precursors for Efficient Metallaphotoredox Couping Reactions

Elevate your photoredox catalysis with our premium radical precursors, meticulously crafted for efficient radical generation via single-electron oxidation! Explore our diverse product lineup, including carboxylic acids, alkylboron derivatives, 1,4-dihydropyridines, and more—ideal for metallaphotoredox systems and coupling reactions.

2025-01-17

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