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NiH-Catalyzed Migratory Defluorinative Olefin Cross-Coupling: Trifluoromethyl-Substituted Alkenes as Acceptor Olefins to Form gem-Difluoroalkenes

We report a NiH-catalyzed migratory defluorinative coupling between two electronically differentiated olefins. A broad range of unactivated donor olefins can be joined directly to acceptor olefins containing an electron-deficient trifluoromethyl substituent in both intra- and intermolecular fashion to form gem-difluoroalkenes. This migratory coupling shows both site- and chemoselectivity under mild conditions, with the formation of a tertiary or quaternary carbon center.

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Intramolecular photocycloaddition of N-alkenyl substituted maleimides: A potential tool for the rapid construction of perhydroazaazulene alkaloids

UV irradiation of a number of N-alkenyl-substituted maleimide derivatives leads to the formation of complex perhydroazaazulenes in excellent yields. The overall process can be considered as a formal intramolecular [5+2] cycloaddition. Substrates were prepared by Mitsunobu coupling of the appropriate alkenols with various maleimides. Methyl substitution of the alkenyl side chain gave the cycloadducts 13a-g in good yields, with moderate to high stereoselectivity being observed for 13e and 13g, respectively. Use of cyclic alkene side chains led to the formation of tri- and tetracyclic products with high degrees of stereoselectivity in most cases. Some of the polycyclic ring systems that were prepared constitute the core skeleton of a number of complex alkaloids. The substrate 29 underwent an unexpected [2+2] photocyclo-addition to yield the unusual cyclobutane 31.

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A new application about 5-Methoxy-3,4-dihydro-2H-pyrrole

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TRICYCLIC INHIBITORS OF THE BCL6 BTB DOMAIN PROTEIN-PROTEIN INTERACTION AND USES THEREOF

The present application relates to compounds of Formula (I) or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting interactions with BCL6 BTB, such as cancer.

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The important role of 1-(4-Methoxyphenyl)-1H-pyrrole-2,5-dione

We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 1081-17-0, and how the biochemistry of the body works.Electric Literature of 1081-17-0

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Simultaneous determination of the content of isoquinoline alkaloids in dicranostigma leptopodum (Maxim) fedde and the effective fractionation of the alkaloids by high-performance liquid chromatography with diode array detection

A simple and efficient method was developed for the simultaneous determination of eight isoquinoline alkaloids in methanol extracts of Dicranostigma leptopodum (Maxim) Fedde and the effective fractionation of the alkaloids of D. leptopodum by high-Performance liquid chromatography with diode array detection. The chromatographic conditions were optimized on a SinoChrom ODS-BP column to obtain a good separation of the four types of alkaloid analytes, including two aporphines (isocorydine, corydine), two protopines (protopine and allocryptopine), a morphine (sinoacutine), and three quaternary protoberberine alkaloids (berberrubine, 5-hydroxycoptisine, and berberine). The separation of these alkaloids was significantly affected by the composition of the mobile phase, and particularly by its pH value. Acetonitrile (A) and 0.2% phosphoric acid solution adjusted to pH 6.32 with triethylamine (B) were selected as the mobile phase with a gradient elution. With this method, a new quaternary protoberberine alkaloid was isolated and the two structural isomers (isocorydine and corydine) were baseline separated. The appropriate harvest period for D. leptopodum was also recommended based on our analysis. The method for the effective fraction of the alkaloids of D. leptopodum was optimized under this method with regard to the varying significant pharmacological activities of the alkaloids.

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Extended knowledge of 1122-10-7

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Application of 1122-10-7, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.1122-10-7, Name is 3,4-Dibromo-1H-pyrrole-2,5-dione, molecular formula is C4HBr2NO2. In a article£¬once mentioned of 1122-10-7

Synthesis and characterization of imine-palladacycles containing imidate “pseudohalide” ligands: Efficient Suzuki-Miyaura cross-coupling precatalysts and their activation to give Pd0Ln species (L = Phosphine)

Dinuclear palladacyclic complexes [{Pd(C^N)(mu-NCO)} 2] (C^N = N-phenylbenzaldimine, Phbz) containing asymmetric imidato units (-NCO- = succinimidate (succ; 1), phthalimidate (phthal; 2), maleimidate (mal; 3), 2,3-dibromomaleimidate (2,3-diBrmal; 4), glutarimidate (glut; 5)) have been readily prepared by reaction between the di-mu-acetate precursor and cyclic imide ligands in a 1:2 molar ratio. Base treatment of the less acidic ligands 2-oxazolidone and delta-valerolactame with KOH/MeOH was required to give analogous -NCO- bridged complexes (6 and 7). Reactions of the dinuclear complexes with tertiary phosphines provide novel mononuclear N-bonded imidate derivatives of the general formula [Pd(Phbz)(imidate)(PR3)] (R = Ph (a), 4-F-C6H4 (b), 4-MeO-C6H4 (c), CH2CH2CN (d)). The application of these novel palladacyclic complexes as precatalysts for the Suzuki-Miyaura cross-coupling reactions of both aryl and benzyl bromides with phenylboronic acid has been examined. The acetate adducts [Pd(Phbz)(CH 3COO)(PR3)] (8a,c) were prepared to assess the role of imidate ligands in catalyst performance. The mononuclear imidate derivatives possess greater activity than the parent dinuclear complexes, exhibiting comparable performance in the cross-coupling of benzyl bromide with arylboronic acids to the best examples reported in the literature. The mononuclear imidate derivatives give a common Pd0Ln intermediate, as inferred by the release of the organic fragment (first reductive elimination product). Catalyst activation occurs by reaction of phenylboronic acid with the palladacycle in the absence of exogenous base (as shown by GC-MS and ESI-MS), with implications for the reliable comparison of catalyst performance across a series of related precatalysts (e.g., how catalyst/reagents are mixed and what is their order of addition). The single-crystal X-ray structures of compounds 4, 7, 1d, 3c, and 8a have been determined.

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A reduction response camptothecin dimer and based on the camptothecin dimer of the reduction-sensitive drug delivery system (by machine translation)

The invention discloses a method for reduction of responding to camptothecin dimer and based on the camptothecin dimer of the reduction-sensitive drug delivery system, which belongs to the biological medicine and medical technology of nanometer. Technical proposal of the invention points are: the dibromo maleic imide sequentially with triethyleneglycol monomethyl ether, 2, 2 – dihydroxymethyl ethyl disulfide, camptothecin reaction reduction response camptothecin dimer, the camptothecin dimer of the structural formula is: The invention also specifically discloses the camptothecin dimer preparing method and based on the camptothecin dimer of the reduction-sensitive drug delivery system. The drug delivery system of this invention with the camptothecin compared with the transmission system, and by the drug loading of 1 wt % increased to 9.6 wt %, and the drug delivery system with a reduced sensitivity, good biocompatibility and inhibit tumor cell proliferation capacity, can be used for preparing with slow controlled release and targeted anticancer drug delivery system. (by machine translation)

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The effects of protopine on physiological characteristics of isolated guinea pig atrium

AIM: To study the effects of protopine(Pro) on physiological characteristics and action machines in isolated guinea pig atria. METHODS: We measured the spontaneous beat, contractility and functional refractory period and observed the effects of Pro on positive staircase phenomenon and post- rest potentiation by using isolated guinea pig atria. RESULTS: Pro obviously inhibited the spontaneous beat and contractive force, prolonged the functional refractory period (FRP) of isolated guinea pig atria. Pro could abolish the positive chronotropic effect of CaCl2. Pro markedly depressed the positive stairease phenomenon induced by increasing the frequency of the electrical pulse and decreased the post-rest potentiation of myocardial contractility in left atria. CONCLUSION: The results suggest that Pro induce inhibitory effects on the spontaneous beat, contractility and prolong the FRP in the atria. The mechanism by which the Pro induce the negative chronotropic and inotropic effects may relate to the inhibition of transmembrane flux of calcium.

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Synthesis and evaluation of a novel fluorescent chemosensor for glutathione based on a rhodamine B and N-[4-(carbonyl) phenyl]maleimide conjugate and its application in living cell imaging

A novel rhodamine B spirolactam derivative bearing an N-[4-(carbonyl)phenyl] maleimide moiety (L1) was designed, synthesized and structurally characterized to develop a chemosensor. The interactions of L1 with amino acids and metal ions were studied by UV?vis absorption and fluorescence spectroscopy. L1 exhibited a highly sensitive and selective turn-on fluorescence response toward glutathione (GSH) over other biological species in EtOH/HEPES (3:2, v/v, 0.1?mM, pH 7.34) solution. The detection limit of GSH by L1 was 0.219?muM. Intracellular imaging applications demonstrated that L1 can be used as a fluorescent probe for the detection of GSH in HepG-2 and HUVEC cells.

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Thermosetting compounds (by machine translation)

Provided is a thermosetting compound which has good solvent solubility, and can be quickly cured by a thermal treatment to form a cured product having ultra-high resistance to heat. The thermosetting compound according to the present invention is represented by formula (1). In formula (1): R1 and R2 each represent a thermosetting group; D1 and D2 are the same or different from each other and each represent a single bond or a linking group; Ar1, Ar2, and Ar3 are the same or different from each other and each represent a divalent aromatic hydrocarbon group, or a divalent group in which two or more aromatic hydrocarbons are bonded together through a single bond, a divalent aliphatic hydrocarbon group, or a divalent alicyclic hydrocarbon group; and E represents an ester bond.

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Catalyst free visible light induced cycloaddition as an avenue for polymer ligation

The current study introduces a tetrazole species able to perform a rapid, visible light induced nitrile imine-mediated tetrazole-ene cycloaddition (NITEC). Full conversion of the tetrazole species under mild, catalyst free conditions is reported. Importantly, the visible light ligation technology is applied as a method for the modification and ligation of polymers featuring the rapid, clean and exclusive formation of the desired cycloadduct.

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