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Synthesis of 2-oxazolidones by sulfur-assisted thiocarboxylation with carbon monoxide and oxidative cyclization with molecular oxygen under mild conditions

Simple synthetic method on 2-oxazolidone derivatives was established. 2-Aminoethanols were easily subjected to the thiocarboxylation with carbon monoxide promoted by elemental sulfur, followed by the oxidative cyclization with molecular oxygen to give corresponding 2-oxazolidones in good yields under mild conditions (1 atm, rt). Furthermore, 2-imidazolidones and 2-thiazolidone were also prepared in good yields similarly.

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Effects of soursop (Annona muricata) leaf water extract (SLWE) on body weight, leptin and TNF alpha plasma levels of rats with high fat and high fructose (HFHF) Diet

Background: Soursop leaves believed to be able to lose weight. The aim of the study was to prove that SLWE had an effect on body weight, leptin and TNF alpha plasma level in mice with the HFHF diet. Methods: The study used post test group design only. Male Wistar rats aged 8-10 weeks weighing 175-200g, healthy, 25 were divided into 5 groups by simple random sampling. Normal groups (N), Positive groups (P) were given a HFHF 10% diet, treatment group (T1), T2, and T3 (HFHF diet + SLWE at dose of 100 mg / kg bw, 200 mg / kg bw, and 400 mg / kg bw). The diet and extract were given for 10 weeks. Measurement of body weight and weighing the amount of food consumed were carried out every week. Measurement of plasma leptin and TNF alpha levels using the ELISA method. Statistical analysis using ANOVA and Kruskal Wallis test with a confidence level p <0.05.Results: SLWE at all doses increased the amount of intake compared to P and N groups (p <0.05).Giving SLWE at dose of 400 mg/kgbw causes a slowdown in weight gain (p> 0.05), increase levels of plasma leptin than P group. There was a tendency to decrease TNF alpha plasma levels with an increase in the dose of the extract (p>0.05). Conclusion: Giving SLWE in HFHF diet-induced mice increased appetite, increased Leptin levels, and tendency to decreased weight gain and TNF alpha levels.

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NOVEL TRICYCLIC COMPOUNDS AS INHIBITORS OF MUTANT IDH ENZYMES

The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes: (I); wherein A is -C(R1)= or -N=; and X is selected from the group consisting of: (II-i), (II-ii), (II-iii), and (II-iv). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.

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Gold-Catalyzed Intermolecular Nitrene Transfer from 2H-Azirines to Ynamides: A Direct Approach to Polysubstituted Pyrroles

(Chemical Equation Presented). An effective gold-catalyzed intermolecular nitrene transfer by the reaction of 2H-azirines and ynamides is reported, which provides highly substituted pyrroles in a straightforward manner. This transformation proceeds under mild conditions and gives the polysubstituted pyrroles in good-to-excellent yields. Preliminary results indicate that a nongold carbenoid pathway is preferred for current pyrrole synthesis.

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Photoreduction of aryl ketones by amides, lactams and various nitrogen-containing heterocycles

Benzophenone is photoreduced by amides and lactams.The hydrogen atom alpha to the nitrogen atom is abstracted regioselectively; coupling of the two resulting radicals leads to adducts with a 1-phenylethanolamide structure.The use of this general reaction in synthetic reactions is demonstrated: adducts of benzophenone with amides, lactams, 2,4-imidazolinediones, tetrahydro-2H-1,3-oxazin-2-one and 2-oxazolidinone, and of dibenzosuberone, 9H-xanthenone, 9H-thioxanthenone and alpha-tetralone with 1-methyl-2-pyrrolidinone, N,N-dimethylacetamide and N,N-diethylacetamide are described.Kinetic parameters for dibenzosuberone and 9H-thioxanthenone are given.Knowledge of the rate constants of photoreduction (kr) and autodeactivation (kTa) allows optimization of the experimental procedure to provide adducts in good yields.

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Catalytic fluoride triggers dehydrative oxazolidinone synthesis from CO2

Herein, catalytic fluoride (F-) is demonstrated to be a trigger for dehydrative immobilization of atmospheric pressure CO2, such that reaction of CO2 with beta-amino alcohols derived from natural amino acids gives optically pure oxazolidinones in high yields. A synergistic combination of fluoride and organosilicon agents (e.g., Bu4NF + Ph3SiF or siloxanes) enhances the catalytic activity and functional group compatibility. This system lies at the interface between homogenous and heterogeneous catalysis, and may prove useful for the development of recoverable/reusable siloxane-based CO2 immobilization materials. This journal is

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THIAZOLE DERIVATIVE

A thiazolylimidazole derivative represented by the formula or a pharmaceutically acceptable salt thereof, and an ALK5 inhibitor, an therapeutic agent for alopecia or a hair growth agent having the above as an active ingredient, wherein: X1 and X2 are different from each other and represent a sulfur atom or a carbon atom; R1 represents a phenyl group; a substituted phenyl group; a phenyl group condensed with a hetero aromatic ring; a pyridyl group; or a pyridyl group condensed with a hetero aromatic ring; R2 represents a hydrogen atom, a halogen atom, an alkyl group having 1 to 6 carbon atoms, an alkyl group having 1 to 6 carbon atoms substituted with 1 to 5 halogen atoms, an alkoxy group having 1 to 6 carbon atoms, an alkanoyl group having 1 to 5 carbon atoms, or a hydroxyalkyl group having 1 to 6 carbon atoms, A represents a group which is represented by the formula. The present invention provides an inhibitory substance against ALK5 which is a TGF-beta type I receptor and provides a hair growth stimulant or a hair growth agent based on its novel activities.

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Structures and properties of mercury(II) coordination polymers

During the last two decades, coordination polymers have received much attention and the number of synthesized compounds is still growing, which is mainly due to their potential application in such fields as microelectronics, nonlinear optics, molecular selection, ion exchange and catalysis. In contrast, coordination polymers of transition metals ions, the formation of polymers with main group metal ions such as mercury(II) is disproportionately sparse when compared with those of other metals. Because of the effects of mercury on environment and its polymers’ applications, it is necessary to understand mercury’s ability to bind donors and form complexes or coordination polymers. This review provides an overview of all the reported coordination polymers of mercury(II) after 1990 and a summary of their properties. One-dimensional polymers, constituted the majority of the mercury(II) coordination polymers and the most frequent coordination number for mercury(II) is four.

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Synthesis of ring-fused oxazolo- and pyrazoloisoquinolinones by a one-pot Pd-catalyzed carboxamidation and aldol-type condensation cascade process

(Chemical Equation Presented) A three-component cascade process is described for the synthesis of ring-fused oxazolo- and pyrazoloisoquinolinones by a one-pot carboxamidation/aldol-type condensation reaction. The cascade process involves Pd-catalyzed carboxamidation of an aryl halide/active methylene compound with oxazolidinone or pyrazolidinone, and subsequent intramolecular base-catalyzed cyclization/dehydration through an aldol-type condensation process, to give ring-fused oxazolo- and pyrazoloisoquinolinones. This methodology provides an easy one-step approach to these important classesof nitrogen-containing heterocycles and can tolerate a wide array of functional groups, including ester, nitrile, methoxy, and halide.

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ELECTRONIC STRUCTURE OF SOME SUBSTITUTED AZOLIDINES. CNDO/2, NMR AND VIBRATIONAL SPECTROSCOPIC STUDIES.

The 1H and 13C chemical shifts, characteristic vibrational frequencies and force constants for some substituted azolidines are correlated with the results of the CNDO/2 calculations.The influence of the exo and endo heteroatoms on the electronic structure of the heterocyclic ring are discussed.

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