- C?H Methylation of Iminoamido Heterocycles with Sulfur Ylides**
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The direct methylation of N-heterocycles is an important transformation for the advancement of pharmaceuticals, agrochemicals, functional materials, and other chemical entities. Herein, the unprecedented C(sp2)-H methylation of iminoamido heterocycles as nucleoside base analogues is described. Notably, trimethylsulfoxonium salt was employed as a methylating agent under aqueous conditions. A wide substrate scope and excellent level of functional-group tolerance were attained. Moreover, this method can be readily applied to the site-selective methylation of azauracil nucleosides. The feasibility of gram-scale reactions and various transformations of the products highlight the synthetic potential of the developed method. Combined deuterium-labeling experiments aided the elucidation of a plausible reaction mechanism.
- Ghosh, Prithwish,Kwon, Na Yeon,Kim, Saegun,Han, Sangil,Lee, Suk Hun,An, Won,Mishra, Neeraj Kumar,Han, Soo Bong,Kim, In Su
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supporting information
p. 191 - 196
(2020/10/29)
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- Direct Conversion of Haloarenes to Phenols under Mild, Transition-Metal-Free Conditions
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A high-yielding and practical method for the synthesis of phenols from electron-deficient haloarenes and heteroarenes has been developed. The products are formed from acetohydroxamic acid as the hydroxide source via a novel SNAr reaction/Lossen rearrangement sequence. Notably, these reactions employ inexpensive and air-stable reagents, require no special handling, occur under mildly basic conditions, and form products in high yields in the presence of electrophilic and protic functionality. The utility of this methodology is demonstrated by the high-yielding hydroxylation of two base-sensitive complex substrates.
- Fier, Patrick S.,Maloney, Kevin M.
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supporting information
p. 2244 - 2247
(2016/06/01)
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- HETEROCYCLIC COMPOUND AND USE THEREOF
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The present invention aims to provide a compound having a PDE inhibitory action and useful as a medicament for the prophylaxis or treatment of schizophrenia and the like. A compound represented by the formula (1x): wherein each symbol is as des
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Paragraph 0665; 0666
(2013/06/05)
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- Synthesis and c-Src inhibitory activity of imidazo[1,5-a]pyrazine derivatives as an agent for treatment of acute ischemic stroke
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We synthesized and evaluated a series of C-5 substituted imidazo[1,5-a]pyrazine derivatives to identify potent c-Src inhibitors as potential therapeutic agents for acute ischemic stroke. Among these compounds, compound 14c·HCl demonstrated remarkable cent
- Mukaiyama, Harunobu,Nishimura, Toshihiro,Kobayashi, Satoko,Ozawa, Tomonaga,Kamada, Noboru,Komatsu, Yoshimitsu,Kikuchi, Shinji,Oonota, Hideki,Kusama, Hiroshi
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p. 868 - 885
(2007/10/03)
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- Novel (substituted phenyl)-1,2,4-triazolo (4,3-A)pyrazines and novel 2-hydrazino-(substituted phenyl)pyrazine intermediates
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This disclosure describes novel 5-,6- and 8-(phenyl and substituted phenyl)-1,2,4-triazolo[4,3-a]pyrazines which posses utility as anxiolytic agents.
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- Some Reactions of Mono Substituted Pyrazine Monoxides
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The reactions of the monoxides of propylpyrazine and phenylpyrazine with phosphoryl chloride or acetic anhydride were investigated.Except in the case of the reaction of 2-propylpyrazine 1-oxide with acetic anhydride, chlorination or acetoxylation occurred
- Ohta, Akihiro,Watanabe, Tokuhiro,Akita, Yasuo,Yoshida, Maki,Toda, Suzumi,et al.
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p. 1061 - 1067
(2007/10/02)
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- 2,3-Diphenyl-5-ethylpyrazine
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The compound 2,3-diphenyl-5-ethyl-pyrazine, useful as a precursor in the synthesis of those compounds of the class of pyrazine, arylpyrazine, diphenylpyrazine, and cycloalkylpyrazine malonates, acetates, acetamides, and acetic acids, useful for their ultraviolet light absorption properties.
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