- Nucleophilic Amination of Methoxy Arenes Promoted by a Sodium Hydride/Iodide Composite
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A method for the nucleophilic amination of methoxy arenes was established by using sodium hydride (NaH) in the presence of lithium iodide (LiI). This method offers an efficient route to benzannulated nitrogen heterocycles. Mechanistic studies showed that the reaction proceeds through an unusual concerted nucleophilic aromatic substitution.
- Kaga, Atsushi,Hayashi, Hirohito,Hakamata, Hiroyuki,Oi, Miku,Uchiyama, Masanobu,Takita, Ryo,Chiba, Shunsuke
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supporting information
p. 11807 - 11811
(2017/09/20)
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- 8-OXOADENINE COMPOUND
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An 8-oxoadenine compound useful as an immuno-modulator having specific activity against Th1/Th2, specifically a prophylactic and therapeutic agent for a topical application for allergic diseases, viral siseases and cancers, which is represented by the following formula (1): , wherein A is a group of a formula represented by the formula (2): , wherein R2 is a substituted or unsubstituted alkyl group and so on, R3 is hydrogen atom or an alkyl group, R is a halogen atom and so on, n is 0-2, X1 is oxygen atom, Z is straight or branched chain alkylene, and R1 is an alkyl group which is optionally substituted by hydroxy group, an alkoxy group, alkoxycarbonyl group and so on, or its pharmaceutically acceptable salt.
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Page/Page column 144
(2010/11/24)
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- Design and Synthesis of New Naphthalenic Derivatives as Ligands for 2-Iodomelatonin Binding Sites
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New melatonin-like agents were designed from the frameworks of 2,5-dimethoxyphenethylamine, an important structural moiety for the 5-HT receptor, and (2-methoxynaphthyl)ethylamine.The compounds were synthesized by classical methods and evaluated in binding assays with chicken brain membranes using 2-(125I>iodomelatonin as the radioligand.Preliminary studies on the series of N-acyl-disubstituted phenethylamines showed the favorable role of the methoxy group in the ortho position of the side chain on the affinity for the receptor ( Ki = 8 +/- 0.2 nM ) for N-propionamide (3o).This effect was confirmed in a series of the naphthalene derivatives, a bioisosteric moiety of the indole ring, and several potent ligands for melatonin binding sites were prepared such as N-propionamide (4b) ( Ki = 0.67 +/- 0.05 nM ) and N-cyclopropylformamide (Ki = 0.05 +/- 0.004 nM ( (4k).Structure-activity relationships are discussed with regard to melatonin and bioisosteric naphthalenic compound 2.The Ki value for 4b was affected to a similar extent to that of melatonin by GTP-γ-S or Mn2+ in competition experiments, suggesting an agonist profile for this compound.
- Langlois, Michel,Bremont, Beatrice,Shen, Shuren,Poncet, Annie,Andrieux, Jean,et al.
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p. 2050 - 2060
(2007/10/02)
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- Autorecycling System for the Specific 1,4-Reduction of α,β-Unsaturated Carbonyl Compounds Catalysed by 1,5-Dihydro-5-deazaflavin
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A useful autorecycling system for the specific 1,4-reduction of α,β-unsaturated carbonyl compounds to the corresponding saturated carbonyl compounds catalysed by a 10-aryl-5-deazaflavin in formic acid is reported.The specific reduction behaviour toward α,β-unsaturated carbonyl compounds is interpreted in terms of frontier molecular orbital theory (PM3 method).
- Nagamatsu, Tomohisa,Kuroda, Kazunori,Mimura, Norio,Yanada, Reiko,Yoneda, Fumio
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p. 1125 - 1128
(2007/10/02)
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