- Transition-Metal-Free C(sp3)a'H Coupling of Cycloalkanes Enabled by Single-Electron Transfer and Hydrogen Atom Transfer
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Here we report a unique transition-metal-free C(sp3)-H/C(sp3)-H coupling of cycloalkanes at room temperature. Unactivated cycloalkanes and 2-azaallyls underwent the combination process of single-electron transfer (SET) and hydrogen atom transfer (HAT) to deliver a wide variety of cycloalkane-functionalized products. This expedient approach enables C(sp3)-H/C(sp3)-H coupling of cycloalkanes under mild conditions without transition metals, initiators, and oxidants.
- Zhang, Linlin,Liu, Zhengfen,Tian, Xun,Zi, Yujin,Duan, Shengzu,Fang, Yongsheng,Chen, Wen,Jing, Hong,Yang, Lijuan,Yang, Xiaodong
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- Method for synthesizing medical intermediates
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The invention discloses a method for synthesizing medical intermediates R-alpha-cyclopentyl (phenyl) methylamine. The particular method includes generating racemization alpha-cyclopentyl (phenyl) methylamine from phenyl cyclopentanone by means of reductiv
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Paragraph 0009
(2017/10/31)
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- Method for synthesizing S-shaped amino compound
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The invention discloses a method for synthesizing S-shaped amino compound, namely, S-alpha-cyclopentyl(phenyl)methylamine. The method includes the steps of using cyclopentyl phenyl ketone as a raw material, allowing cyclopentyl phenyl ketone to react with
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- BICYCLIC HETEROCYCLE DERIVATIVES AND USE THEREOF AS GPR119 MODULATORS
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The present invention relates to Bicyclic Heterocycle Derivatives of formula (I), compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR1 19 in a patient.
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Page/Page column 161
(2009/12/27)
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- Synthesis and structure-activity relationships of potential anticonvulsants based on 2-piperidinecarboxylic acid and related pharmacophores
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Using N-(2,6-dimethyl)phenyl-2-piperidinecarboxamide (1) and N-(α-methylbenzyl)-2-piperidinecarboxamide (2) as structural leads, a variety of analogues were synthesised and evaluated for anticonvulsant activity in the MES test in mice. In the N-benzyl series, introduction of 3-Cl, 4-Cl, 3,4-Cl2, or 3-CF3 groups on the aromatic ring led to an increase in MES activity. Replacement of the α-methyl group by either i-Pr or benzyl groups enhanced MES activity with no increase in neurotoxicity. Substitution on the piperidine ring nitrogen led to a decrease in MES activity and neurotoxicity, while reduction of the amide carbonyl led to a complete loss of activity. Movement of the carboxamide group to either the 3- or 4-positions of the piperidine ring decreased MES activity and neurotoxicity. Incorporation of the piperidine ring into a tetrahydroisoquinoline or diazahydrinone nucleus led to increased neurotoxicity. In the N-(2,6-dimethyl)phenyl series, opening of the piperidine ring between the 1- and 6-positions gave the active norleucine derivative 75 (ED50 = 5.8 mg kg-1, TD50 = 36.4 mg kg-1, PI = 6.3). Replacement of the piperidine ring of 1 by cycloalkane (cyclohexane, cyclopentane, and cyclobutane) resulted in compounds with decreased MES activity and neurotoxicity, whereas replacement of the piperidine ring by a 4-pyridyl group led to a retention of MES activity with a comparable PI. Simplification of the 2-piperidinecarboxamide nucleus of 1 into a glycinecarboxamide nucleus led to about a six-fold decrease in MES activity. The 2,6-dimethylanilides were the most potent compounds in the MES test in each group of compounds evaluated, and compounds 50 and 75 should be useful leads in the development of agents for the treatment of tonic-clonic and partial seizures in man.
- Ho, Bin,Michael Crider,Stables, James P
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p. 265 - 286
(2007/10/03)
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- Hypoglycemic α cycloalkylphenylmethyl, furanalkyl, and thiophenealkyl lactamimides
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A series of α cycloalkylphenylmethyl lactamimides and a series of furan and thiophenealkyl lactamimides were prepared for biological evaluation as an extension of earlier findings of hypoglycemic activity in lactamimides. Several compounds produced pronouced hypoglycemia after oral administration to fasted, glucose primed rats.
- Grisar,Claxton,Wiech
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p. 365 - 369
(2007/10/04)
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