TBHP Promotes Cross-Dehydrogenative Coupling of SF Alkynes with Tetrahydroisoquinolines under Copper Catalysis.

We present a viable approach for the cross-dehydrogenative coupling of Het-SF-alkynes with tetrahydroisoquinolines under oxidative conditions, using TBHP and copper catalysts. These newly developed conditions boast enhanced yields and a more extensive range of substrates, demonstrating tolerance to various functional groups and addressing the limitations of earlier reports. Consequently, this method should increase opportunities for the exploration of SF-containing compounds and their potential applications in drug discovery, materials science, and as alternatives to PFAS.

Expanding the Frontier of Linear Drug Design: Cu-Catalyzed C -C -Coupling of Electron-Deficient SF -Alkynes with Alkyl Iodides.

Despite the attractive properties of tetrafluorosulfanyl (SF ) compounds in drug discovery, medicinal research on SF molecules is hindered by the scarcity of suitable synthetic methodologies. Drawing inspiration from the well-established Sonogashira cross-coupling of terminal alkynes under Pd-catalysis, it is envisioned that SF -alkynes can serve as effective coupling partners. To overcome the challenges associated with the electron-deficient nature of SF -alkynes and the lability of the SF unit under transition-metal catalysis, an aryl radical mediated C -C cross-coupling reaction is successfully developed under Cu catalysis.

Investigating the Antibacterial Effects of Synthetic Gamma-Lactam Heterocycles on Methicillin-Resistant Strains and Assessing the Safety and Effectiveness of Lead Compound MFM514.

Methicillin-resistant (MRSA) continues to be one of the main causes of hospital-acquired infections in all regions of the world, while linezolid is one of the only commercially available oral antibiotics available against this dangerous gram-positive pathogen. In this study, the antibacterial activity from 32 analogues of synthetic gamma-lactam heterocycles against MRSA was determined. Amongst screened analogues for the minimum inhibitory concentration (MIC) assay, compound displayed good inhibitory activity with MIC values of 7.

-Ethyl -(2,3,4)-4-hy-droxy-1,2-dimethyl-5-oxopyrrolidine-3-carboxyl-ate.

The asymmetric unit of the title compound, CHNO, consists of a functionalized pyrrolidine ring having an envelope conformation, synthesized as an ethyl ester. The mol-ecule has three chiral centres and crystallized as a racemic mixture. In the crystal, mol-ecules are linked by pairwise O-H⋯O bonds, generating dimers with twofold rotational symmetry.