Hua-Li Qin

An efficient one‐pot method for the synthesis of α ‐arylcycloalkenes from cyclic ketones and aryl Grignard reagents has been developed. Concentrated hydrochloric acid is added directly to the crude Grignard addition mixture at room temperature, which quenches the excess organomagnesium reagent and affords the α ‐arylcycloalkene without isolation of intermediates. The method accommodates several electronically diverse aryl Grignard reagents and various cyclic ketones, including seven‐ and eight‐membered cyclic ketones, as well as heteroatom‐containing and fused‐ring substrates, providing the desired products in moderate to excellent yields. The reaction can also be performed on gram scales.

Sulfonyl fluorides have emerged as versatile building blocks in organic synthesis and click chemistry, driving a strong demand for efficient synthetic methods. However, the cost‐effective and straightforward synthesis of these compounds remains challenging. Herein, we report a practical one‐pot protocol that directly converts commercially available thiols or disulfides into sulfonyl fluorides using trichloroisocyanuric acid (TCCA) as an inexpensive chlorinating oxidant. This transition‐metal‐free method features operational simplicity, mild conditions, retention of the substrate skeleton, and broad substrate scope, offering a robust and accessible platform for the rapid assembly of structurally diverse sulfonyl fluoride building blocks.

Sulfonamides are privileged structural motifs widely found in bioactive molecules and pharmaceuticals. Their derivatives exhibit excellent structural diversity, a feature proven useful for discovering novel therapeutic agents.

A chemoselective [4 + 2] annulation protocol employing 2-aminostyrylsulfonyl fluoride and isothiocyanates was established, enabling selective access to two distinct classes of 3,1-benzothiazine- and tetrahydroquinazoline-functionalized sulfonyl fluorides. This method provides a novel approach for constructing highly functionalized sulfonyl fluoride pharmacophores that hold significant potential in the fields of medicinal chemistry, chemical biology, and drug discovery.

Lung cancer cause of cancer fatalities around the world.

Breast cancer is among the most prevalent malignancies affecting women globally.

An efficient hydrodehalogenation method was developed using RANEY® nickel as the catalyst. In aqueous media, various aryl halides could be efficiently reduced to the corresponding arenes in excellent yields with H ₂ as the reductant.