- One-Pot Sequential Multistep Transformation of α,β-Unsaturated Trifluoromethyl Ketones: Facile Synthesis of Trifluoromethylated 2-Pyridones
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A one-pot transformation of α,β-unsaturated trifluoromethyl ketones with 2-(phenylsulfinyl)acetamide to give trifluoromethylated 2-pyridones is realized. The reaction proceeds under mild conditions and involves multiple steps in an expeditious and controlled sequence to provide efficient access to a broad range of trifluoromethylated 2-pyridones in moderate to high yields. Moreover, further synthetic manipulations permit the routine synthesis of a diverse array of trifluoromethylated pyridines with good efficiency.
- Lv, Ning,Tian, Yi-Qiang,Zhang, Fa-Guang,Ma, Jun-An
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supporting information
p. 605 - 609
(2019/03/07)
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- Direct access to α-sulfenylated amides/esters: Via sequential oxidative sulfenylation and C-C bond cleavage of 3-oxobutyric amides/esters
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An efficient, environmentally benign and unprecedented synthesis of various α-sulfenylated amides/esters has been developed under oxygen atmosphere. The reaction shows good functional group tolerance and excellent chemo/regioselectivity. All the desired products were obtained in moderate to excellent yields, even on the gram scale. Practically, the related α-thiol Weinreb amide can be readily transferred to a series of prospective compounds, and selenium atom can be introduced to the α-sites of the amides in high yields.
- Jiang, Yi,Deng, Jie-Dan,Wang, Hui-Hong,Zou, Jiao-Xia,Wang, Yong-Qiang,Chen, Jin-Hong,Zhu, Long-Qing,Zhang, Hong-Hua,Peng, Xue,Wang, Zhen
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supporting information
p. 802 - 805
(2018/02/06)
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- HYDROXAMIC ACID DERIVATIVES AND HDAC8 INHIBITORS
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PROBLEM TO BE SOLVED: To provide compounds that are highly active and can highly selectively inhibit HDAC8 functionality, and HDAC8 inhibitors. SOLUTION: Each hydroxamic acid derivative comprise a compound of the general formula (1) in the figure, where φ
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Paragraph 0025; 0028
(2016/10/07)
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- Design, synthesis, and biological activity of NCC149 derivatives as histone deacetylasea 8-selective inhibitors
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We recently discovered N-hydroxy-3-[1-(phenylthio)methyl-1H-1,2,3-triazol- 4-yl]benzamide (NCC149) as a potent and selective histone deacetylasea 8 (HDAC8) inhibitor from a 151-member triazole compound library using a click chemistry approach. In this wor
- Suzuki, Takayoshi,Muto, Nobusuke,Bando, Masashige,Itoh, Yukihiro,Masaki, Ayako,Ri, Masaki,Ota, Yosuke,Nakagawa, Hidehiko,Iida, Shinsuke,Shirahige, Katsuhiko,Miyata, Naoki
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p. 657 - 664
(2014/03/21)
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- Synthesis and biological evaluation of 2-Phenoxyacetamide analogues, a novel class of potent and selective monoamine oxidase inhibitors
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Monoamine oxidases (EC 1.4.3.4; MAOs), a family of FAD-containing enzymes, is an important target for antidepressant drugs. In this paper, a series of 2-phenoxyacetamide analogues were synthesized, and their inhibitory potency towards monoamine oxidases A (MAO-A) and B (MAO-B) were evaluated using enzyme and cancer cell lysate. 2-(4-Methoxyphenoxy)acetamide (compound 12) (SI = 245) and (2-(4-((prop-2- ynylimino)methyl)phenoxy)acetamide (compound 21) (IC50MAO-A = 0.018 μM, IC50MAO-B = 0.07 μM) were successfully identified as the most specific MAO-A inhibitor, and the most potent MAO-A/-B inhibitor, respectively. The inhibitory activities of these two compounds in living cells were also further evaluated utilizing HepG2 and SHSY-5Y cell lysates.
- Shen, Wei,Yu, Shian,Zhang, Jiaming,Jia, Weizheng,Zhu, Qing
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p. 18620 - 18631
(2015/01/08)
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- 2-pyridone synthesis using 2-(phenylsulfinyl)acetamide
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2-Pyridones were prepared by means of an efficient protocol including the 1,4-addition of 2-(phenylsulfinyl)acetamide to α,β-unsaturated ketones followed by cyclization and sulfoxide elimination.
- Fujii, Masaya,Nishimura, Takuya,Koshiba, Takahiro,Yokoshima, Satoshi,Fukuyama, Tohru
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supporting information
p. 232 - 234
(2013/04/10)
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- Direct catalytic formation of primary and tertiary amides from non-activated carboxylic acids, employing carbamates as amine source
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The operationally simple titanium(IV)- or zirconium(IV)-catalyzed direct amidation of non-activated carboxylic acids with ammonium carbamates generates primary, and tertiary N,N-dimethyl-substituted amides in good to excellent yields. Copyright
- Tinnis, Fredrik,Lundberg, Helena,Adolfsson, Hans
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supporting information
p. 2531 - 2536
(2012/11/06)
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