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A compound of formula (I) or a pharmaceutically acceptable salt or ester thereof, wherein R1 to R8, A1 to A3 have the significance given in claim 1, can be used as AMPK modulators for treating obesity, hyperglycemia or type 2 diabetes.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H88NO – PubChem

 

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We describe in this Letter the synthesis of an original thymine azido-heterotrimer generated by Click Chemistry. This trimer has been obtained from an azido-thymidine and a new chloroethyl-propargylated PNA monomer analogue, after two azidation/click-reaction cycles. Conformational preferences of a rotameric intermediate have also been studied.

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Oxazolidine – Wikipedia,
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Mild, efficient, copper-catalyzed N-arylation procedures for nitrogen heterocycles, amides, carbamates, and C-arylation procedures for malonic acid derivatives have been developed that afford high yields of arylated products with excellent selectivity. The N-arylation of imidazole with aryl bromides or iodides was found to be greatly accelerated by inexpensive, air-stable catalyst systems, combining catalytic copper salts or oxides with a set of structurally simple chelating ligands. The reaction was shown to be compatible with a broad range of aryl halides, encompassing sterically hindered, electron-poor, and electron-rich ones, providing the arylated products under particularly mild conditions (50-82C). The lower limit in ligand and catalyst loading and the scope of Ullmann-type condensations catalyzed by complexes bearing those ligands with respect to the nucleophile class have also been investigated. Chelating Schiff base Chxn-Py-Al (1c) generates a remarkably general copper catalyst for N-arylation of pyrrole, indole, 1,2,4-triazole, amides, and carbamates; and C-arylation of diethyl malonate, ethyl cyanoacetate, and malononitrile with aryl iodides under mild conditions (50-82C). The new method reported here is the most successful to date with regard to Ullmann-type arylation of some of these nucleophiles.

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Oxazolidine – Wikipedia,
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Potassium alkoxides of N-acyl-oxazolidin-2-one-syn-aldols undergo stereoselective elimination reactions to afford a range of trisubstituted (E)-alphabeta-unsaturated amides in >95% de, that may be subsequently converted into their corresponding (E)-alphabeta-unsaturated acids or (E)-alphabeta-unsaturated oxazolines in good yield. syn-Aldols derived from alphabeta-unsaturated aldehydes gave their corresponding trisubstituted (E)-alphabeta-unsaturated-amides with poorer levels of diastereocontrol, whilst there was a similar loss in (E)-selectivity during elimination of syn-aldols derived from chiral aldehydes. These elimination reactions proceed via rearrangement of the potassium alkoxide of the syn-aldol to a 1,3-oxazinane-2,4-dione enolate intermediate that subsequently eliminates carbon dioxide to afford a trisubstituted (E)-alphabeta-unsaturated amide. The (E)-selectivity observed during the ElcB-type elimination step has been rationalised using a simple conformational model that employs a chair-like transition state to explain the observed stereocontrol. The Royal Society of Chemistry 2005.

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The stereochemical course of the oxidation of chiral oxazolidinone-substituted enecarbamates has been studied for singlet oxygen (1O2), dimethyldioxirane (DMD), and m-chloroperbenzoic acid (mCPBA) by examining of the special structural and stereoelectronic features of the enecarbamates. Valuable mechanistic insight into these selective oxidations is gained. Whereas the R1 substituent on the chiral auxiliary is responsible for the steric shielding of the double bond and determines the sense of the pi-facial diastereoselectivity, structural characteristic such as the Z/E configuration and the nature of the R 2 group on the double bond are responsible for the extent of the diastereoselectivity. Stereoelectronic steering by the vinylic nitrogen functionality controls the mode selectivity (ene reaction vs [2+2] cycloaddition) in the case of 1O2.

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As part of our efforts to develop agents for cognitive enhancement, we have been focused on the 5-HT6 receptor in order to identify potent and selective ligands for this purpose. Herein we report the identification of a novel series of 3-sulfonylindazole derivatives with acyclic amino side chains as potent and selective 5-HT6 antagonists. The synthesis and detailed SAR of this class of compounds are reported.

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Simple, reproducible and detailed preparations of S-<2-(3-aminopropyl)aminoethyl> and S-<2-(3-N-methylaminopropyl)aminoethyl> phosphorothioic acids (HO)2P(O)-S-(CH2)2-NH-(CH2)3-NH-R (R=H and CH3), named WR 2721 and WR 1680 respectively, are described.The yields of each step have been optimized to facilitate the synthesis of these compounds of large interest in the cancer radio- and chemotherapy.

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CO2 capture and storage are quite a promising approach to limit greenhouse gas emission. However CO2 capture process relies on the use of amine solutions which are likely to degrade and produce potentially harmful compounds. To ensure an environmental acceptance and to understand this degradation, analytical methods are needed to identify and quantify as many as possible of these products. In our study, monoethanolamine was used as a model compound for CO2 capture. Therefore an analytical strategy was developed to provide the most exhaustive list of degradation products. It was based on the complementarity between liquid and gas chromatography coupled with various mass spectrometry ionization and detection modes.. This analytical strategy enabled the identification of 59 degradation products in pilot plant samples, but 26 of which were never reported. It provides also key information to develop quantification methods for pilot or industrial plant monitoring.

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The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras

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Bromoalkanoate imides undergo intramolecular alkylation to form cyclopentane carboximides using catalytic amounts of magnesium bromide in the presence of DBU. Addition of PyBox ligands affords alkylation products with moderate enantioselectivity.

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