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Nitroimidazoles: Part V – 1-(1-Methyl-5-nitroimidazol-2-yl)-1,2,4-triazolidin-3,5-diones and Analogues

Condensation of 1-methyl-2-methylsulphonyl-5-nitroimidazole (1) with the sodium salts of triazolindiones affords the derivatives 2a-i; similiar reaction with the sodium salts of thiazolidinone, 2-iminothiazolidine, pyrrolidinone, oxazolidinone and its 2-methyl and 2-chloromethyl analogues leads to the formation of products 3-8 respectively.Under the reaction conditions 3 is opened by dimethylamide ion to form 10, and 6 by methyl sulfinate ion to provide 13 respectively.Additionally, 6 is hydrolysed to the amine (12).Cyclic sulphamides undergo reaction with 1 to provide nitroimidazoles (23-28).

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Carbon dioxide induced degradation of diethanolamine during absorption and desorption processes

Alkanolamines are widely used in the purification of the sour gas sweetening process. During the sour gas absorption process, CO2 significantly degrades the amine solvent and creates enormous problems for plant operation. In this work, CO2 induced degradation of aqueous diethanolamine (DEA) solution was conducted in a 1.25 L jacketed glass reactor that functioned as an absorber and stripper at atmospheric conditions. Pure CO2 was bubbled through the reactor until the solution became saturated. In this study, the concentrations of DEA used were in the range of concentrations between 2 mol¡¤L? 1 and 4 mol¡¤L? 1. In the degradation experiment, six generic cycles were conducted for each run. Each cycle was configured with the absorption and desorption of carbon dioxide at 55 C and 100 C, respectively. Samples were collected after a predetermined experimental time and analyzed by ion chromatography (IC) to identify unknown ionic degradation products (DGPs). In the IC analysis, three different columns were used for anion, cation and ion exclusion systems, which are Metrosep A Supp 5 150/4.0, Metrosep C Supp 4 150/4.0 and Metrosep Organic Acids, respectively. The major identified DGPs of D01DEA2M, D02DEA3M, and D03DEA4M are nitrite, acetate and ammonium. Phosphate product was found in the degraded amine samples which might be due to the contamination of water or chromatographic system.

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A simple one-pot preparation of N-allenyl amides, ureas, carbamates and sulfonamides using a DMSO/tBuOK protocol

A one-pot transformation of amides, ureas, carbamates and sulfonamides into synthetically useful N-allenyl analogues using a tBuOK/DMSO protocol is reported. The procedure is experimentally simple and robust, and provides N-allenyl analogues, commonly used within the literature, in yields comparable to the benchmark two-step approach.

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Oxazolidine – Wikipedia,
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Direct N-acylation of lactams, oxazolidinones, and imidazolidinones with aldehydes by Shvo’s catalyst

Direct N-acylation of lactams, oxazolidinones, and imidazolidinones was achieved with aldehydes by Shvo’s catalyst without using any other stoichiometric reagent. The N-acylations with alpha,beta-unsaturated aldehydes were achieved with excellent yields.

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DERIVATIVES OF 2-[2-(BENZO- OR PYRIDO-) THIAZOLYLAMINO]-6-AMINOPYRIDINE, USEFUL IN THE TREATMENT OF RESPIRATORIC, ALLERGIC OR INFLAMMATORY DISEASES

The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular Itk activity

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The Dichotomy of Gold-catalyzed Interplay between Cyanamides and Ynamides: Controllable Switch from [2+2+2] to [4+2] Cycloaddition

The gold-catalyzed interplay between cyanamides and ynamides demonstrates condition-dependent mechanistic dichotomy. [2+2+2] Cycloaddition proceeds under kinetically controlled conditions to give 2,4,6-triaminopyrimidines (19 examples, up to 99%). Under thermodynamically controlled conditions, the reactivity switches from [2+2+2]- to [4+2] cycloaddition; the latter [4+2] reaction accomplishes 1,3-diaminoisoquinolines (19 examples, up to 97%). The advantages of both methods include regioselectivity, mild reaction conditions (even for the thermodynamically controlled [4+2] reaction) and the possibility of introducing a variety of dialkyl, diaryl, and heterocyclic amino substituents into the target pyrimidine and isoquinoline cores. The reactions were conducted on gram scales and the versatility of the obtained products was demonstrated by post-functionalizations. (Figure presented.).

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2-(1-HETEROARYLPIPERAZIN-4-YL)METHYL-1,4-BENZODIOXANE DERIVATIVES AS ALPHA2C ANTAGONISTS

Compounds of formula I (formula I), wherein A is an optionally substituted five-membered unsaturated heterocyclic ring containing 1, 2 or 3 N, O or S ring heteroatom(s) exhibit alpha2C antagonistic activity and are thus useful for the treatment of diseases or conditions of the peripheric or central nervous system.

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Oxazolidine – Wikipedia,
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Highly efficient KF/Al2O3-catalyzed versatile hetero-Michael addition of nitrogen, oxygen, and sulfur nucleophiles to alpha,beta-ethylenic compounds

The first example of KF/Al2O3-catalyzed versatile hetero-Michael addition reaction of nitrogen, oxygen, and sulfur nucleophiles was developed for facile preparation of organic compounds of widely different structures. In contrast with the existing methods using many acidic catalysts, this method is very general, simple, high-yielding, environmentally friendly, and oxygen and moisture tolerant.

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Visible-Light-Mediated Liberation and In Situ Conversion of Fluorophosgene

The first example for the photocatalytic generation of a highly electrophilic intermediate that is not based on radical reactivity is reported. The single-electron reduction of bench-stable and commercially available 4-(trifluoromethoxy)benzonitrile by an organic photosensitizer leads to its fragmentation into fluorophosgene and benzonitrile. The in situ generated fluorophosgene was used for the preparation of carbonates, carbamates, and urea derivatives in moderate to excellent yields via an intramolecular cyclization reaction. Transient spectroscopic investigations suggest the formation of a catalyst charge-transfer complex-dimer as the catalytic active species. Fluorophosgene as a highly reactive intermediate, was indirectly detected via its next downstream carbonyl fluoride intermediate by NMR. Furthermore, detailed NMR analyses provided a comprehensive reaction mechanism including a water dependent off-cycle equilibrium.

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Synthesis of some 2-Oxazolidinones in mild conditions

One step efficient protocol for the synthesis of 2-oxazolidinones in paste chemical medium is described under microwave activation with 80 % yield.

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