28394-58-3Relevant academic research and scientific papers
Synthesis, spectral characterization, and biological studies of 3,5-disubstituted-1,3,4-oxadiazole-2(3H)-thione derivatives
?zyazici, Tug?e,Sahin, Fikrettin,K?ksal, Meri?
, p. 749 - 760 (2021/07/26)
The reaction of 3,4-dichlorophenyl-1,3,4-oxadiazole-2(3H)-thione with piperidine derivatives via Mannich reaction was used to generate eleven novel compounds in moderate to good yields. Synthesized molecules were characterized according to their structure
Design, synthesis, insecticidal activity and 3D-QSR study for novel trifluoromethyl pyridine derivatives containing an 1,3,4-oxadiazole moiety
Xu,Wang,Luo,Yu,Guo,Fu,Zhao,Wu
, p. 6306 - 6314 (2018/02/19)
A series of trifluoromethyl pyridine derivatives containing 1,3,4-oxadiazole moiety was designed, synthesized and bio-assayed for their insecticidal activity. The result of bio-assays indicated the synthesized compounds exhibited good insecticidal activity against Mythimna separata and Plutella xylostella, most of the title compounds show 100% insecticidal activity at 500 mg L-1 and >80% activity at 250 mg L-1 against the two pests. Compounds E18 and E27 showed LC50 values of 38.5 and 30.8 mg L-1 against Mythimna separata, respectively, which were close to that of avermectin (29.6 mg L-1); compounds E5, E6, E9, E10, E15, E25, E26, and E27 showed 100% activity at 250 mg L-1, which were better than chlorpyrifos (87%). CoMFA and CoMSIA models with good predictability were proposed, which revealed the electron-withdrawing groups with an appropriate bulk at 2- and 4-positions of benzene ring could enhance insecticidal activity.
Some Novel Mannich Bases of 5-(3,4-Dichlorophenyl)-1,3,4-oxadiazole-2(3H)-one and Their Anti-Inflammatory Activity
Koksal, Meric,Ozkan-Dagliyan, Irem,Ozyazici, Tugce,Kadioglu, Beril,Sipahi, Hande,Bozkurt, Ayhan,Bilge, Suleyman S.
, (2017/09/05)
Non-steroidal anti-inflammatory drugs (NSAIDs), which are widely used for the treatment of rheumatic arthritis, pain, and many different types of inflammatory disorders, cause serious gastrointestinal (GI) side effects. The free carboxylic acid group exis
Metal-free aerobic oxidative esterification of aldehydes in the presence of cyanide
Kim, Yoo-Jin,Cheon, Cheol-Hong
supporting information, p. 2055 - 2061 (2015/08/18)
A metal-free aerobic oxidative esterification of aldehydes in the presence of cyanide is described. Various aromatic aldehydes and sterically congested alcohols were amenable to this protocol. In addition, this method could be extended to the preparation of thioesters with a thiol in place of an alcohol. Furthermore, the cyanide-mediated aerobic oxidation of aldehydes was applied to the synthesis of lactones via intramolecular esterification in the absence of an alcohol.
Direct conversion of aromatic ketones to arenecarboxylic esters via carbon-carbon bond-cleavage reactions
Yin, Guodong,Gao, Meng,Wang, Zihua,Wu, Yandong,Wu, Anxin
experimental part, p. 369 - 372 (2009/04/07)
Aromatic methyl ketones, ss-keto esters, and trifluoromethyl-l,3- diketones can be directly converted to arene-carboxylic esters via carbon-carbon bond cleavage of pyridinium iodide intermediates in the presence of copper(II) oxide, iodine, pyridine, and potassium carbonate in alcoholic media. The advantages of the present method in terms of good yields, mild reaction conditions, and inexpensive reagents should make this protocol a valuable alternative to the existing methods.
Synthesis, characterization and anti-inflammatory activity of new 5- (3,4-dichlorophenyl)-2-(aroylmethyl) thio-1,3,4-oxadiaxoles
Koksal, Meric,Bilge, S. Sirri,Bozkurt, Ayhan,Sahin, Z. Sibel,Isik, Samil,Erol, Dilek Demir
experimental part, p. 510 - 514 (2009/04/05)
Several 5-(3,4-dichlorophenyl)-2-(aroylmethyl)thio-1,3,4-oxadiazoles were synthesized and characterized by elemental analyses, IR and nuclear magnetic resonance spectra. All compounds were evaluated for anti-inflammatory activity by determining their abil
Domino N-H/C-H bond activation: Palladium-catalyzed synthesis of annulated heterocycles using dichloro(hetero)arenes
Ackermann, Lutz,Althammer, Andreas
, p. 1627 - 1629 (2008/02/13)
(Chemical Equation Presented) One after the other: A novel palladium-catalyzed domino reaction consisting of an amination and a direct C-H bond arylation allows for a general synthesis of annulated heterocycles starting from readily available 1,2-dichloroarenes and primary as well as secondary anilines (see scheme; Cy = cyclohexyl). This is high-lighted by an efficient synthesis of the natural product murrayafoline A.
PHENYL-[4-(3-PHENYL-1H-PYRAZOL-4-YL)-PYRIMIDIN-2-Yl)-AMINE DERIVATIVES
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Page 44, (2010/11/30)
The invention relates to phenyl-[4-(3-phenyl-1H-pyrazol-4-yl)-pyrimidin-2-yl)-amine derivatives and to processes for the preparation thereof, to pharmaceutical compositions comprising such derivatives and to the use of such derivatives - alone or in combination with one or more other pharmaceutically active compounds - for the preparation of pharmaceutical compositions for the treatment especially of a proliferative disease, such as a tumour.
Relative reactivity of methyl iodide to ethyl iodide in nucleophilic substitution reactions in acetonitrile and partial desolvation accompanying activation
Kondo, Yasuhiko,Urade, Miyuki,Yamanishi, Yukari,Chen, Xinyu
, p. 1449 - 1454 (2007/10/03)
Through the examination of empirical correlations involving activation parameters for nucleophilic substitution of methyl iodide and of ethyl iodide, nucleophiles have been classified into three series: (1) nucleophiles with two equivalent reaction sites, (2) nucleophiles with a chlorine atom in the para-position, and (3) nucleophiles with a single reaction site. Three types of partial desolvation processes accompanying activation have been deduced on the basis of these classifications. A major factor determining the relative reactivity of methyl iodide to ethyl iodide in the substitution reaction of an anionic nucleophile having a single reaction site in acetonitrile (kMeI/kEtI) is suggested to be partial desolvation around the nucleophilic center on going from reactant to transition-state.
Synthesis of dibenzoylmethane derivatives and inhibition of mutagenicity in Salmonella typhimurium
Choshi,horimoto,Wang,Nagase,Ichikawa,Sugino,Hibino
, p. 1047 - 1049 (2007/10/02)
Twenty dibenzoylmethanes with methyl, methoxy, bromo, chloro, or fluoro substitution on either one or both benzene rings were synthesized and assayed for inhibition of the mutagenicity of 2-nitrofluorene in S. typhimurium TA98. 2,2-Dimethoxy, 3,3-dimethoxy and 3,3,4,4-tetramethoxydibenzoylmethane was as active as dibenzoylmethane. None of the halogen-substituted dibenzoylmethanes were active. These results demonstrate that dibenzoylmethanes can inhibit the mutagenicity of 2-nitrofluorene, and that modifications made on the benzene rings of dibenzoylmethane cannot enhance the antimutagenicity of this parent compound.
