1,2-Oxaborines: Unlocking Molecular Core Diversity for Drug Discovery

Recently, Professor Guangbin Dong and his team at the University of Chicago have reported a conceptually different approach in Nature Chemistry that allows rapid access to diverse core structures from a common intermediate using 1,2-oxaborines as a versatile molecular platform. A soft enolization/6π-electrocyclization strategy has been developed to synthesize 1,2-oxaborines from readily available enones or enals efficiently. Taking advantage of their multifaceted reactivities, 1,2-oxaborines can undergo further C−H functionalization and be transformed into a diverse range of arenes, heteroarenes and non-aromatic heterocycles. The corresponding key reagents and building blocks are now in stock at AmBeed, and we hope this advancement inspires your ongoing work.

2025-11-07

Decoding Cellular Senescence: From Molecular Mechanisms to Cutting-Edge Intervention Strategies

Cellular senescence is a multifaceted state of stable growth arrest triggered by diverse intracellular and extracellular stressors, representing a systemic homeostatic response that coordinates the clearance of damaged cells and tissue regeneration. Cellular senescence can be classified into two principal types: replicative senescence and stress-induced premature senescence [1].

2025-11-05

Photocatalytic Oxygen-Atom Transmutation in Oxetanes

Recently, the research group of Ph.D. Ming Joo Koh at the National University of Singapore, in collaboration with Dr. Xinglong Zhang at the Chinese University of Hong Kong, published a paper in Nature entitled "Photocatalytic oxygen-atom transmutation of oxetanes"[1]. This work achieves a breakthrough in oxygen-atom replacement of oxetanes. Their developed photocatalytic strategy selectively substitutes the endocyclic oxygen atom, transforming it in a single step into diverse nitrogen-, sulfur-, or carbon-bridged four-membered and five-membered saturated cyclic systems. The mechanism involves a photocatalytic ring-opening process that forms a dihalide intermediate, followed by nucleophile-mediated ring closure to complete the "atom transmutation"(Fig. 1b). This method exhibits excellent functional group compatibility and chemoselectivity, is applicable for late-stage modification of complex bioactive molecules, and provides a more straightforward route for the synthesis of pharmaceuticals and their analogues.

2025-10-29

One-Step C-to-N Swap: Direct Magic Conversion of Indoles to Benzimidazoles

Recently, the group of Bill Morandi at ETH Zürich has unveiled a novel “C-to-N swap” strategy for N-alkyl indoles: at room temperature in methanol, using commercially available PIDA (phenyliodine(III) diacetate) as oxidant and H₂NCO₂NH₄ as nitrogen source, the protocol converts indoles into the corresponding benzimidazoles in a one-pot process within only 30 minutes. The reaction leverages the innate reactivity of the indole scaffold to engage in an initial oxidative cleavage step, followed by oxidative amidation, Hofmann-type rearrangement and cyclization. The reaction tolerates a wide range of functional groups, which is demonstrated by the interconversion of 15 drug-like molecules. The work is reported in Nat. Chem.

2025-10-21

Stereo- reversed E2 unlocks Z- selective C–H functionalization

Recently, Researchers from the University of Wisconsin–Madison, led by Professor Zachary K. Wickens, have published an article titled "Stereo-reversed E2 unlocks Z-selective C–H functionalization" in Science. The study describes the transformation of alkenes into transient 1,2- bis- sulfonium intermediates found to undergo Z- selective elimination, overturning a textbook E2 stereoselectivity rule through stabilizing interactions. Researchers identify paired electrolysis as an enabling strategy to both selectively generate the requisite bis- sulfonium intermediate and drive its rapid elimination in situ. the resultant Z- alkenyl sulfonium linchpins provide access to a wide array of Z- alkene targets from inexpensive feedstocks through robust cross- coupling reactions.

2025-10-14

Decoding Signalling Pathways in Hepatocellular Carcinoma: Emerging Targets and Therapeutic Strategies (Part.I)

Hepatocellular carcinoma (HCC), the predominant form of liver cancer, remains one of the most challenging malignancies, ranking sixth in global incidence and third in cancer-related mortality.

2025-10-13

Fe-Thiol Photocatalyzed Direct Decarboxylative Hydroalkylation: One-Step CF₃-Small-Ring Olefin Assembly

Recently, Prof. Dr. D. Katayev and Prof. Dr. J. G. West reported a catalytic approach for the direct decarboxylation of challenging CF3-cyclopropyl and cyclobutyl carboxylic acids using cooperative iron-thiol catalysis. This strategy enables the efficient generation of valuable radicals that can be incorporated into activated and unactivated alkenes, offering access to elusive chemical space. The corresponding key reagents and starting materials are now in stock at AmBeed, and we hope this advancement inspires your ongoing work.

2025-09-25

Revitalizing reformatsky reagent for catalyst-free direct alkylation with unactivated alkyl halides

Reformatsky reagents (generated from α-halo carbonyl compounds and zinc) have traditionally been primarily employed in reactions with activated electrophiles such as aldehydes, ketones, acyl chlorides, etc. These reagents are known for their lower reactivity compared to organolithium or Grignard reagents. Due to their limited nucleophilicity, they generally cannot undergo direct nucleophilic substitution (SN₂) with unactivated alkyl halides (e.g., ethyl bromide) and typically require reliance on transition metal catalysis (e.g., Ni, Fe, Co, etc.).

2025-09-23

Decoding Prostate Cancer: Drug Resistance And Precision Medicine (Part II)

Last week, we presented an overview of prostate cancer development, targeted therapeutic strategies, and the core molecular mechanism—the androgen receptor (AR) signalling pathway. This installment explores the mechanisms of drug resistance in prostate cancer and targeted treatment strategies for bone metastasis.

2025-09-22

Site-selective Ru-catalysed saturation of unactivated arenes via directed 6π activation

On August 28, 2025, the Guangbin Dong group at the University of Chicago unveiled a new strategy for arene hydrogenation! For the first time, directed-group-controlled, site-selective saturation of unactivated arenes has been realized: under Ru catalysis, the arene adjacent to the directing group is hydrogenated with exceptional precision, tolerating 20+ sensitive functional groups—including alkenes and aryl bromides—with exclusive cis-selectivity of >20:1 and gram-scale yields, up to 85%. The method has already enabled a streamlined synthesis of the antimalarial agent cis-atovaquone (obtained in a single step from commercial starting material), providing a powerful tool for “escaping from flatland” in drug molecules.

2025-09-10

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