- Generation of Dimethyl Sulfoxide Coordinated Thermally Stable Halogen Cation Pools for C?H Halogenation
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A method to generate halogen cation pools from the reaction of 1,2-dihaloethanes (hal=Br, I) and dimethyl sulfoxide (DMSO) for C?H halogenation of arenes and heteroarenes was reported. The initial reaction of DMSO and 1,2-dihaloethane generates the sulfur
- Dalai, Pallaba Ganjan,Palit, Kuntal,Panda, Niranjan
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supporting information
p. 1031 - 1038
(2022/02/02)
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- Hypervalent iodane mediated reactions of: N -acetyl enamines for the synthesis of oxazoles and imidazoles
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A hypervalent iodane reagent used for the intramolecular cyclization of N-acetyl enamines and intermolecular cyclocondensation of enamines and nitriles was investigated. The reaction was performed under mild conditions and gave oxazoles and imidazoles, respectively, in moderate to excellent yields. This transformation exhibits good reactivity, selectivity and functional group tolerance. The selectivity of the intra- or intermolecular reaction is dependent on the structure of N-acetyl enamines.
- Xu, Kang,Yang, Ruiqi,Yang, Shuang,Jiang, Cheng,Ding, Zhenhua
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p. 8977 - 8981
(2019/10/28)
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- OPIOID RECEPTOR MODULATORS AND USE THEREOF
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Disclosed is an in vitro screening method for identifying an antagonist-to-agonist allosteric modifier of a mu-opioid receptor and an in vivo method for confirming that a test compound is such a modifier of a mu-opioid receptor. Also disclosed is a method
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Paragraph 0355; 0356; 0357
(2017/03/21)
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- 4,6-DIARYLAMINOTHIAZINES AS BACE1 INHIBITORS AND THEIR USE FOR THE REDUCTION OF BETA-AMYLOID PRODUCTION
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Compounds of formula (I), including pharmaceutically acceptable salts thereof, are set forth herein: (I) wherein R1 and R2 are independently hydrogen, or -CH3; or R1 and R2 can join together in a ring by adding -(CH2)4-; R3 is hydrogen or C1-C3 al-kyl; Y and Z are independently a C6-C10- aryl group or a 5-10 membered heterocyclic group which can be further substituted with from 0-3 substituents selected from the group of halogen, hydroxy, amino, C1-4 alkylamino, C1-4 dialkylamino, halo C1-4 alkyl, CN, C1-C6, alkyl or cycloalkyl, C1-C6 alkoxy, -C=OC1-4 alkyl, -SO2C1-4 alkyl, and C2-C4 alkynyl; A is selected from the group of phenyl, ben-zyl, oxazolyl, thiazolyl, isoxazolyl, imidazolyl, pyrazolyl, pyridyl, pyrimidinyl, and pyrazinyl groups which can be further substituted with from 0-3 substituents selected from the group of halogen, hydroxy, amino, C1-4 alkylamino, C1-4 dialkylamino, haloC1-4 alkyl, hydroxyC1-6 alkyl, CN, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, and C2-C4 alkynyl; L is -NHCO-, or is a single bond; and L and Z to-gether can be absent
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- Synthesis of oxazoles from enamides via phenyliodine diacetate-mediated intramolecular oxidative cyclization
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A group of functionalized oxazoles were synthesized in moderate to good yields from enamides via phenyliodine diacetate (PIDA)-mediated intramolecular cyclization. The main advantageous features of the present method include its broad substrate scope and the heavy-metal-free characteristic of the oxidative carbon-oxygen bond formation process.
- Zheng, Yunhui,Li, Xuming,Ren, Chengfeng,Zhang-Negrerie, Daisy,Du, Yunfei,Zhao, Kang
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p. 10353 - 10361
(2013/01/15)
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- Gold catalysis: Phenol synthesis in the presence of functional groups
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The effect of different substituants, such as bromo, chloromethyl, hydroxymethyl, formyl, acetyl, carboxy, and acylated hydroxymethyl and ammonium groups, on the furan ring of substrates in gold-catalyzed phenol synthesis has been investigated. The furan
- Hashmi, A. Stephen K.,Weyrauch, Jan P.,Kurpejovic, Elzen,Frost, Tanja M.,Miehlich, Burkhard,Frey, Wolfgang,Bats, Jan W.
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p. 5806 - 5814
(2008/03/11)
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- The Effect of Ring Nitrogen Atoms on the Homolytic Reactivity of Phenolic Compounds: Understanding the Radical-Scavenging Ability of 5-Pyrimidinols
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Six substituted 5-pyrimidinols were synthesized, and the thermochemistry and kinetics of their reactions with free radicals were studied and compared to those of equivalently substituted phenols. To assess their potential as hydrogen-atom donors to free r
- Valgimigli, Luca,Brigati, Giovanni,Pedulli, Gian Franco,DiLabio, Gino A.,Mastragostino, Marina,Arbizzani, Catia,Pratt, Derek A.
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p. 4997 - 5010
(2007/10/03)
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- Efficient synthesis of multi-substituted oxazoles under solvent-free microwave irradiation
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A new and efficient method for the synthesis of multi-substituted oxazoles from various carbonyl compounds has been developed using sequential treatment of carbonyl compounds with HDNIB and amides such as acetamide or benzamide under solvent-free microwave irradiation conditions.
- Lee, Jong Chan,Choi, Hyun Jung,Lee, Yong Chan
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p. 123 - 125
(2007/10/03)
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- Novel chain-breaking antioxidants
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Compounds, preferably 5-pyrimidinol and 3-pyridinol derivatives, that act as effective chain breaking antioxidants of both the lipid and water-soluble variety (analogous to the natural Vitamins E and C), many of which are more reactive toward peroxyl radicals than the most potent form of Vitamin E. These compounds may exhibit many chemopreventive effects associated with conditions in which free radical-mediated cellular damage or disruption is implicated and Vitamins E and C are shown to have protective effects. Additionally, these compounds should be excellent oxidation inhibitors as additives to fuels, lubricants, rubber, polymers, chemicals, solvents and foodstuffs.
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- REACTIONS OF OXAZOLES WITH ACETYLENE DERIVATIVES. PART III. REACTIONS OF TRISUBSTITUTED OXAZOLE DERIVATIVES WITH ETHYL PROPIOLATE
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Diene reactions between dimethyloxazoles containing an electron accepting group in positions 2 or 5 with ethyl propiolate were investigated.The formation of both possible, isomeric furan derivatives was stated in the case of all these reactions.The ratio of both products depends on the kind of the electron accepting group and does not depend on the places of methyl and electron accepting groups in positions 2 and 5 in the oxazole.
- Jaworski, Tadeusz,Mizerski, Tadeusz
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