36207-13-3Relevant academic research and scientific papers
Synthesis and bioactivity of sulfide derivatives containing 1,3,4-oxadiazole and pyridine
Yu, Gang,Chen, Shunhong,He, Feng,Luo, Dexia,Zhang, Yu,Wu, Jian
, p. 1075 - 1085 (2019/09/10)
A series of novel sulfide derivatives containing 1,3,4-oxadiazole and pyridine were synthesized, characterized, and tested for their antibacterial activity against tobacco bacterial wilt and rice bacterial blight and for insecticidal activity toward diamondback moth. The results showed that some compounds had good insecticidal and bactericidal activity, e.g., the activities of compounds 6e and 6g–6j toward tobacco bacterial wilt were much better than those of commercial thiodiazole-copper, and some of the synthesized compounds possessed good insecticidal activity against Plutella xylostella. Compounds 6d, 6h, 6j, 6l, 6p, 6r, and 6p displayed over 93% activity at 500 mg L? 1.
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.
Facile, highly efficient and environmentally friendly transesterification mediated by platinum dioxide and nickel oxide under essentially neutral conditions
Teng, Binhao,Shi, Jiangong,Yao, Chunsuo
supporting information, p. 2465 - 2471 (2018/06/11)
A practical, facile and highly efficient transesterification reaction under essentially neutral conditions was achieved using platinum dioxide (PtO2) or PtO2/nickel oxide (NiO) as the catalyst. A number of esters and alcohols that contain various functional groups were employed. Good to excellent yields were obtained for different aromatic or aliphatic starting materials. The Pt-alcohol intermediate generated in situ facilitated the exchange of low-alcohol esters to high-alcohol esters.
Single electron transfer-induced coupling of alkynylzinc reagents with aryl and alkenyl iodides
Okura, Keisho,Kawashima, Hitomi,Tamakuni, Fumiko,Nishida, Naoya,Shirakawa, Eiji
supporting information, p. 14019 - 14022 (2016/12/09)
Alkynylzinc reagents were found to undergo coupling with aryl and alkenyl iodides to give arylalkynes and alkenylalkynes without the aid of transition metals. The coupling reaction proceeds through a single electron transfer mechanism, where a substoichiometric amount of a phosphine works as an indispensable activator.
A general and efficient suzuki-miyaura cross-coupling protocol using weak base and no water: The essential mole of acetate
Wang, Bing,Sun, Hui-Xia,Sun, Zhi-Hua
experimental part, p. 3688 - 3692 (2009/12/03)
A weak base, CsOAc, promotes Suzuki-Miyaura cross-coupling and related Pd-catalyzed reactions under anhydrous conditions as effectively as stronger bases. Aryl triflates exhibit unusual reaction rates, which are comparable to that: of bromoarenes. A negle
Diacylhydrazine derivatives as novel potential chitin biosynthesis inhibitors: Design, synthesis, and structure-activity relationship
Ke, Shaoyong,Qian, Xuhong,Liu, Fengyi,Wang, Ni,Fan, Feng,Li, Zhong,Yang, Qing
experimental part, p. 2985 - 2993 (2009/10/02)
A series of diacylhydrazine derivatives containing hydrophobic alkyl chains have been designed and synthesized. The target molecules have been identified on the basis of analytical spectral (IR, 1H NMR, 13C NMR, and HRMS) data. All synthesized compounds have been screened for their potential inhibition in vitro against chitin synthesis using yeast cell extracts. The preliminary assays indicate that some of the compounds display moderate to good inhibitory activity. Structure-activity relationship (SAR) is also discussed based on the experimental data, and the further analysis of the quantitative structure-activity relationship (QSAR) indicates that the electronic parameter is the main factor to affect inhibition activities.
Novel 4H-1,3,4-oxadiazin-5(6H)-ones with hydrophobic and long alkyl chains: Design, synthesis, and bioactive diversity on inhibition of monoamine oxidase, chitin biosynthesis and tumor cell
Ke, Shao-Yong,Qian, Xu-Hong,Liu, Feng-Yi,Wang, Ni,Yang, Qing,Li, Zhong
scheme or table, p. 2113 - 2121 (2009/10/02)
A new series of nitrogen-containing heterocycles 4H-1,3,4-oxadiazin-5(6H)-ones derivatives with hydrophobic and long chains were designed and synthesized by direct cyclization reaction of N′-alkylation substituted aroylhydrazines with chloroacetyl chloride. The preliminary assays showed that some of the compounds displayed moderate to good inhibitory activities toward monoamine oxidase (MAO) at the concentration of 10-5-10-3 M, and antitumor activities against human lung cancer A-549 and human prostate cancer PC-3 cell lines at μM level, which might provide new scaffold for anticancer agents. Furthermore, compounds 5i and 5m exhibited significant inhibitory activity on chitin biosynthesis, which might represent a novel class of highly potential inhibitors of chitin synthesis. Crown Copyright
1,3,4-Oxadiazoline derivatives as novel potential inhibitors targeting chitin biosynthesis: Design, synthesis and biological evaluation
Ke, Shaoyong,Liu, Fengyi,Wang, Ni,Yang, Qing,Qian, Xuhong
scheme or table, p. 332 - 335 (2011/02/26)
Two series of 1,3,4-oxadiazoline heterocycle derivatives were designed, synthesized and identified. Bioactivity assays showed that all synthesized compounds inhibited chitin synthesis in yeast, suggesting they might be a novel class of potential inhibitors against chitin biosynthesis. The structure-activity relationships (SAR) of these compounds are discussed.
Palladium-catalyzed cross-coupling reaction of tricyclopropylbismuth with aryl halides and triflates
Gagnon, Alexandre,Duplessis, Martin,Alsabeh, Pamela,Barabe, Francis
, p. 3604 - 3607 (2008/09/20)
(Chemical Equation Presented) The palladium-catalyzed cross-coupling reaction of tricyclopropylbismuth with aryl and heterocyclic halides and triflates is reported. The reaction tolerates numerous functional groups and does not require anhydrous conditions. The method was successfully extended to the cross-coupling of triethylbismuth.
Addition reactions and redox esterifications of carbonyl compounds by N-heterocyclic carbenes of indazole
Schmidt, Andreas,Habeck, Tobias,Snovydovych, Bohdan,Eisfeld, Wolfgang
, p. 3515 - 3518 (2008/02/11)
Thermal decarboxylation converts 1,2-dimethylindazolium-3-carboxylate into indazol-3-ylidene, which reacts in situ with ketones to form stable 1:1 adducts. When the reaction is conducted with aromatic aldehydes in alcohols, redox esterifications to benzoates are observed. Model reactions such as redox esterifications of aromatic aldehydes with sodium alcoholates in the presence of 1,2-dimethylindazolium salt and oxidations of sodium benzylates by 1,2-dimethylindazolium salt to aldehydes lend support to a Cannizzaro-type mechanism of this reaction.
