Highly Selective Perfluoroalkylation of Unsaturated Molecules upon Photoirradiation in BTF as an Organic/Fluorous Hybrid Solvent

Benzotrifluoride (BTF), an eco-friendly solvent, can dissolve many organic and fluorous molecules because of the organic and fluorous motifs in its structure. Using BTF as solvent, we have developed a series of reactions for perfluoroalkylation of various unsaturated compounds upon photoirradiation with a Xe lamp through Pyrex. For example, alkynes, allenes, vinylcyclopropanes, isocyanides, diynes, dienes, and enynes successfully undergo regioselective perfluoroalkyliodination, perfluoroalkylselenation, and perfluoroalkyltelluration in BTF. In addition, the present photoinitiation procedure can be applied to trifluoromethylatio

Development of Kupffer cell targeting type-I interferon for the treatment of hepatitis via inducing anti-inflammatory and immunomodulatory actions

Because of its multifaceted anti-inflammatory and immunomodulatory effects, delivering type-I interferon to Kupffer cells has the potential to function as a novel type of therapy for the treatment of various types of hepatitis. We report herein on the preparation of a Kupffer cell targeting type-I interferon, an albumin-IFNα2b fusion protein that contains highly mannosylated N-linked oligosaccharide chains, Man-HSA(D494N)-IFNα2b, attached by combining albumin fusion technology and site-directed mutagenesis. The presence of this unique oligosaccharide permits the protein to be efficiently, rapidly and preferentially distributed to Kupffer cells. Likewise IFNα2b, Man-HSA(D494N)-IFNα2b caused a significant induction in the mRNA levels of IL-10, IL-1Ra, PD-L1 in RAW264.7 cells and mouse isolated Kupffer cells, and these inductions were largely inhibited by blocking the interferon receptor. These data indicate that Man-HSA(D494N)-IFNα2b retained the biological activities of type-I interferon. Man-HSA(D494N)-IFNα2b significantly inhibited liver injury in Concanavalin A (Con-A)-induced hepatitis model mice, and consequently improved their survival rate. Moreover, the post-administration of Man-HSA(D494N)-IFNα2b at 2 h after the Con-A challenge also exerted hepato-protective effects. In conclusion, this proof-of-concept study demonstrates the therapeutic effectiveness and utility of Kupffer cell targeting type-I interferon against hepatitis via its anti-inflammatory and immunomodulatory actions

Synthesis of Aromatic Carbonyl Thiourea PI-28 Derivatives for the Development of Radicle Elongation Inhibitor of Parasitic Weeds

Aromatic carbonyl thiourea PI-28 has been focused on as a lead compound for the developing radicle elongation inhibitors in germinating Orobanche minor dry seeds. In this study, we have synthesized PI-28 and its derivatives using commercially available phenols, 2-chloroacetamide, and aryl isothiocyanates. In this method, 2-aryloxyacetanilides, which are also attractive as bioactive compounds, were obtained as byproducts. These compounds were formed due to the loss of isothiocyanate moiety from the formed aromatic carbonyl thioureas

A Facile and Rapid Access to Resveratrol Derivatives and Their Radioprotective Activity

A facile and rapid access to resveratrol derivatives has been achieved based on palladium-catalyzed oxidative Heck reaction of aryl moronic acids with styrenes followed by demethylation in moderate to good yields. A series of resveratrol derivatives with various functional groups has been synthesized easily. The radio protective activity of synthesized compounds has also been evaluated using rat thymocytes. The results revealed that some resveratrol derivatives efficiently protected the thymocytes from radiation-induced apoptosis

Proline-Mediated Transition Metal-Free Access to 1<i>H</i>‑Indazolones from 2‑Halobenzohydrazides

Transition metal-free access to 1<i>H</i>-indazolones <b>1</b> has been achieved on the basis of base-mediated intramolecular C–N bond formation. Reactions of 2-halobenzohydrazides <b>2</b> with potassium <i>tert</i>-butoxide in the presence of catalytic proline provided indazolones <b>1</b> in moderate to good yields. This transformation may proceed primarily via the radical pathway according to the control experiment with a radical scavenger

Catalytic C–H/olefin coupling

Abstract -Several ruthenium complexes have been found to catalyze the addition of the C-H bond of arenes to olefins. Phenyl methyl ketone undergoes addition at its ortho position across the double bond of trimethylvinylsilane in the presence of a catalytic amount of RuH2(CO)(PPh3)3 to give 1 : 1 and 1 : 2 coupling products. In the latter, the two ortho hydrogens have reacted. Similarly, 2-methylphenyl methyl ketone reacts with trimethylvinylsilane and triethoxyvinylsilane to give t h e corresponding 1 : 1 coupling products in virtually quantitative yields. The results represent a breakthrough in the chemistry of carbon-hydrogen bond cleavage by metal complexes