123440-85-7Relevant articles and documents
Synthesis method of 2-acetylpyridine
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Paragraph 0017-0018; 0020-0021; 0023-0024, (2020/03/06)
The invention provides a synthesis method of 2-acetylpyridine. The synthesis method comprises the following steps: carrying out a condensation reaction on ethyl 2-picolinate and tert-butyl acetate under alkaline conditions to obtain tert-butyl 2-pyridylacetate, further carrying out hydrolysis in a sulfuric acid solution with a concentration of 20%, and carrying out deacidification to obtain 2-acetylpyridine. The preparation method has the beneficial effects that since a better leaving group, i.e., a tert-butyl group, is adopted, reaction yield is greatly improved, good effect is achieved, andhigh yield is achieved.
Design, synthesis and RON receptor tyrosine kinase inhibitory activity of new head groups analogs of LCRF-0004
Raeppel, Franck,Raeppel, Stéphane L.,Therrien, Eric
, p. 3810 - 3815 (2015/08/24)
New heteroarylcarboxamide head groups substituted with two aromatic rings analogs of thieno[3,2-b]pyridine-based kinase inhibitor LCRF-0004 were designed and synthesized. Potent inhibitors of RON tyrosine kinase with various level of selectivity for c-Met RTK were obtained.
Improved gelatinase a selectivity by novel zinc binding groups containing galardin derivatives
Auge, Franck,Hornebeck, William,Decarme, Martine,Laronze, Jean-Yves
, p. 1783 - 1786 (2007/10/03)
The synthesis of several analogues of galardin, a MMP inhibitor, are presented with their in vitro inhibitory activity against MMP-1 and MMP-2. These compounds contain a distinct Zinc Binding Group (ZBG). Those having a 2-acylated-heterocycle as well as a 2-arylamide function do not exhibit a good inhibition/selectivity against the enzymes tested. On the contrary, those that are based on a hydrazide scaffold present potent selectivity for MMP-2 versus MMP-1.
Studies on non-thiazolidinedione antidiabetic Agents. 2. Novel oxyiminoalkanoic acid derivatives as potent glucose and lipid lowering agents
Imoto, Hiroshi,Sugiyama, Yasuo,Kimura, Hiroyuki,Momose, Yu
, p. 138 - 151 (2007/10/03)
We previously reported that (Z)-2-{4-[(5-methyl-2-phenyl-1,3-oxazol-4-yl) methoxy]benzyloxyimino}-2-(4-phenoxyphenyl)acetic acid (3) showed potent glucose and lipid lowering effects in genetically obese and diabetic mice, KKA y. This compound a
Preparation of N-Silyl-enamines from α-Silyl Carbanions and Aromatic Nitriles
Konakahara, Takeo,Kurosaki, Yoshihiro
, p. 1068 - 1086 (2007/10/02)
The preparations of seven N-silyl-enamines (1a) - (1g) and their chemical behaviour are reported.Lithiated 4-(trimethylsilylmethyl)pyridine (2b) easily reacted with benzonitrile (4a) in tetrahydrofuran to give only (E)-1-phenyl-2-(4-pyridyl)-1-(trimethylsilylamino)ethene (1b) in 90percent yield.On the other hand, lithiated t-butyl trimethylsilylacetate (2c) did not react with (4a) at all, but reacted readily with 2- or 4-cyanopyridines, (4b) or (4c), and scarcely at all reacted with 3-cyanopyridine (4d) to give the corresponding t-butyl (Z)-3-trimethylsilylamino-3-pyridylpropenoates (1c), (1d), and (1e) in 68, 75, and 4percent yields, respectively.The reaction of 3-methyl-5-(trimethylsilylmethyl)isoxazole (2d) with the nitriles (4a) or (4b) gave the corresponding N-silyl-enamine (1g) or the desilylated enamines (5b,c), which were unstable and were readily hydrolyzed to the corresponding ketones (6a) or (6b).