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Several new sulfamidocarbonyloxyphosphonates were prepared in two steps, namely carbamoylation and sulfamoylation, by using chlorosulfonyl isocyanate (CSI), alpha-hydroxyphosphonates, and various amino derivatives and related (primary or secondary amines, beta-amino esters, and oxazolidin-2-ones). All structures were confirmed by 1H, 13C, and 31P NMR spectroscopy, IR spectroscopy, and mass spectroscopy, as well as elemental analysis. Eight compounds were evaluated for their in vitro antibacterial activity against four reference bacteria including Gram-positive Staphylococcus aureus (ATCC 25923), and Gram-negative Escherichia coli (ATCC 25922), Klebsiella pneumonia (ATCC 700603), Pseudomonas aeruginosa (ATCC 27853), in addition to three clinical strains of each studied bacterial species. Compounds 1a?7a and 1b showed significant antibacterial activity compared to sulfamethoxazole/trimethoprim, the reference drug used in this study.

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The C-N cross-coupling reaction between aromatic halides and amides has now been applied to 2- and 3-substituted bromofurans and bromothiophenes. Catalytic CuI in the presence of N,N?-dimethylethylenediamine as a ligand and K3PO4 or K2CO3 as the base furnished 2- and 3-substituted amidofurans and thiophenes ranging from 11 to 99% depending on the particular amide source used.

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The present invention is directed to tricyclic compounds of formula (I), pharmaceutically acceptable compositions comprising compounds of the invention and said compositions for use in methods for the treatment of various disorders in particular cancer.

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The dehydrative condensation of 1,2-aminoalcohols with CO2 is found to proceed in NMP as solvent; 2-oxazolidinones are obtained in the yields of 53-94% when a commercially available tin compound, n-Bu2SnO is used as catalyst.

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Piperazinyl oxoalkyl tetrahydroisoquinolines and related analogues of the Formula: are provided, in which variables are as described herein. Such compounds may be used to modulate ligand binding to histamine H3 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) and other disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting histamine H3 receptors (e.g., receptor localization studies).

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An improved procedure for the three-component coupling reaction of aldehydes, amides, and dienophiles (AAD-reaction) has been developed. The use of microwave technology enables the endo-selective synthesis of N-acyl cyclohexenylamines via condensation of readily available aldehydes and amides, and subsequent Diels-Alder reaction with electron-deficient dienophiles in significantly improved yields. Advantageously, there is no need of employing additional solvents and reaction times are drastically reduced compared to similar thermal reactions.

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This manuscript describes a highly enantioselective conjugate hydrazine addition to alpha,beta-unsaturated imides. The achiral template used has a significant impact on product enantioselectivity. Reactions at lower temperatures provide a protocol to add substituted hydrazines with selectivity resulting in the formation of a single pyrazolidinone product (>98:2 selectivity). A variety of chiral pyrazolidinones with potential as chiral auxiliaries and ligands are accessible through the new conjugate addition methodology. Copyright

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Small neutral carbonyl compounds (2-5) form very stable complexes (Ka’s ranging from 1E3 to 1E5 M-1) with ethyl 2,6-diaminonicotinium tetrakis(3,5-bis(trifluoromethyl)phenyl)borate (1) in dichloromethane.The dominant driving force for complexation between the host and guest.

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Di(2-ethylhexyl) phthalate (DEHP) is the most common phthalate ester, which has been used as a plasticizer for the production of numerous polymers, particularly polyvinyl chloride (PVC). Many other groups have synthesized meso-DEHP indicating interest in this molecule, but we are the first to synthesize enantiomerically pure di[(R)-2-ethylhexyl] phthalate. We report herein, for the first time, the isolation-from the cultures of Bacillus thuringiensis, B. subtilis, and B. velezensis strains-of di[(R)-2-ethylhexyl] phthalate, enantiomerically pure and in good yields: its biological activity against bacteria and fungi was probed and for the first time its synthesis was done.

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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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