Syntheses of Acridones via Copper(II)-Mediated Relay Reactions from <i>o</i>‑Aminoacetophenones and Arylboronic Acids

The reaction of <i>o</i>-aminoacetophenones and arylboronic acids catalyzed by copper­(II) salts in the presence of pyridine under an O₂ atmosphere provides a general and efficient one-pot preparation of biologically interesting acridones. This relay reaction comprises an intermolecular Suzuki cross-coupling, intramolecular oxidative C­(sp³)–H amination, and C­(sp²)–H activation with simultaneous rearrangement of the generated isatin intermediates. This strategy tolerates both electron-donating and -withdrawing functionalities to afford various acridones in good to excellent yields

Iron-Catalyzed Intramolecular C(<i>sp</i>²)–N Cyclization of 1‑(<i>N</i>‑Arylpyrrol-2-yl)ethanone <i>O</i>‑Acetyl Oximes toward Pyrrolo[1,2‑<i>a</i>]quinoxaline Derivatives

An efficient and convenient iron-catalyzed protocol has been developed for the synthesis of substituted pyrrolo­[1,2-<i>a</i>]­quinoxalines from 1-(<i>N</i>-arylpyrrol-2-yl)­ethanone <i>O</i>-acetyl oximes through N–O bond cleavage and intramolecular directed C–H arylation reactions in acetic acid

Synthesis of Multisubstituted Pyrroles from Doubly Activated Cyclopropanes Using an Iron-Mediated Oxidation Domino Reaction

An alternative route has been developed for the construction of multisubstituted pyrrole derivatives from readily available, doubly activated cyclopropanes and anilines using an iron-mediated oxidation domino reaction (i.e., sequential ring-opening, cyclization, and dehydrogenation reactions). This reaction uses readily available reactants and is tolerant of a broad range of substrates, with the desired products being formed in good to excellent yields

Optimal conditions of purified rhLY and hLY for their antibacterial activity.

<p>(A) The optimal temperatures of the rhLY and hLY against <i>M</i>. <i>lysodeikticus</i> were measured in phosphate buffered saline (pH 7.18) at 25°C, 40°C, 60°C, and 80°C respectively. (B) The optimal pH values of the rhLY and hLY for the antibacterial activity was measured in phosphate buffer with different pH values (from 2–12), separately. hLY, commercial hLY; rhLY, purified rhLY. The experiment for each group was repeated at least three times, and the results were presented as mean ± S.D.</p

Expression of rHLY in transgenic chickens.

<p>(A) RT-PCR analysis of the expression of rhLY in G3 and G4 hens. Total RNA was isolated from the heart, liver, spleen, lung, kidney, intestine and oviduct of the G3 and G4 hens. NC (negative control) was the RNA of the oviduct from a non-transgenic hen. The 460bp fragments represented the RT-PCR products of hLY, and the 81bp fragments represented the RT-PCR products of GAPDH. M, DNA ladder. (B) Western blot of egg whites from a G3, a G4 and a non-transgenic hen (NC). Samples were separated by SDS-PAGE and hybridized with anti-hLY antibody and anti-cLY antibody, separately. hLY, commercial hLY (positive control for anti-hLY); cLY, commercial cLY (positive control of anti-cLY).</p

Immunofluorescence detection of hLY expression in oviduct sections.

<p>Sections of the magnum portions of the oviducts from a G3, a G4, and a wild type White Leghorn hen were immunolabeled with the anti-hLY antibody (red). The nuclei were stained with DAPI (blue). Scale bar: 25 μm.</p

Stability of purified rhLY and hLY under different pH conditions.

<p>The lysozyme was incubated in phosphate buffer of different pH values (from 2–12) for 20 minutes. Then the antibacterial activity against <i>M</i>. <i>lysodeikticus</i> was measured in phosphate buffered saline (pH 7.18) at room temperature. The lysozyme activity incubated in phosphate buffer at pH 7 was defined as 100% activity. hLY, commercial hLY; rhLY, purified rhLY. The experiment for each group was repeated at least three times, and the results were presented as mean ± S.D.</p

Antibacterial activity of rhLY, hLY, and cLY against <i>M</i>. <i>lysodeikticus</i>.

<p>The picture showed the inhibition zones of the agar disc diffusion of commercial hLY (A), commercial cLY (B), purified rhLY (C), and sterile water (D, negative control).</p

Thermostability of purified rhLY and hLY at 100°C, 80°C and 60°C.

<p>The lysozyme samples were first incubated for different periods of time at 100°C (A), 80°C (B), and 60°C (C), and their antibacterial activity against <i>M</i>. <i>lysodeikticus</i> was measured in phosphate buffered saline (pH 7.18) at room temperature. Lysozyme activity without heat treatment was defined as 100% activity. hLY, commercial hLY; rhLY, purified rhLY. The experiment for each group was repeated at least three times, and the results were presented as mean ± S.D.</p

Copper-Catalyzed Difunctionalization of Allenes with Sulfonyl Iodides Leading to (<i>E</i>)‑α-Iodomethyl Vinylsulfones

A highly regioselective iodosulfonylation of allenes in the presence of CuI and 1,10-phenanthroline has been developed for the synthesis of various useful (<i>E</i>)-α-iodomethyl vinylsulfones in moderate to excellent yields. This practical reaction is fast, operationally simple, and in particular, proceeds under very mild conditions to afford the target products with high regio- and stereoselectivity. The selectivity was illustrated by a conceptual DFT analysis