33499-42-2Relevant articles and documents
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.
Tirfluoromethylpyridine oxadiazoles (ether)derivative and application thereof
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Paragraph 0162-0164, (2018/07/30)
The invention discloses an application of a tirfluoromethylpyridine oxadiazole (ether)derivative in a pesticide. A structure is shown as a general formula I, a compound shown in the general formula Ihas good insecticidal activity, and can be used for controlling insects such as diamondback moth and armyworm. The compound has excellent control effect for insects such as diamondback moth and armyworm, and also has control effect for the insects having resistance to the traditional pesticides, in addition, introduction of fluorine-containing groups such as tirfluoromethylpyridine and oxadiazoleas well as heterocyclic ring can enhance a rate for forming hydrogen bond effect between a compound and a target, and the activity of the compound is increased.
COMPOSITIONS AND METHODS FOR TREATING FRIEDREICH'S ATAXIA
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Paragraph 0206, (2016/04/19)
The invention provides compositions and methods useful for the treatment of Friedreich's ataxia. In some embodiments, the invention provides compositions and methods useful for inhibiting the ubiquitination of frataxin.
Acid Chloride Synthesis by the Palladium-Catalyzed Chlorocarbonylation of Aryl Bromides
Quesnel, Jeffrey S.,Kayser, Laure V.,Fabrikant, Alexander,Arndtsen, Bruce A.
supporting information, p. 9550 - 9555 (2015/06/30)
We report a palladium-catalyzed method to synthesize acid chlorides by the chlorocarbonylation of aryl bromides. Mechanistic studies suggest the combination of sterically encumbered PtBu3 and CO coordination to palladium can rapidly equilibrate the oxidative addition/reductive elimination of carbon-halogen bonds. This provides a useful method to assemble highly reactive acid chlorides from stable and available reagents, and can be coupled with subsequent nucleophilic reactions to generate new classes of carbonylated products. The Good, the Bad and the Bulky! By employing a sterically encumbered phosphine ligand, tri-tert-butyl phosphine, under palladium catalysis inert aryl bromides are chlorocarbonylated to create reactive acid chlorides by reversible carbon-halogen bond reductive elimination. This general platform allows for an expanded scope of the Heck carbonylation reaction to include previously incompatible nucleophiles.
Linear self-eliminating oligomers
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, (2009/12/07)
The present invention relates to a linear self-eliminating oligomer comprising one or more cleavable triggers, linker units, effector units and a carrier, and a pharmaceutical composition comprising said oligomer.
Synthesis of novel heteroarotinoids with receptor activation capabilities and tgase activity. Single crystal analysis of (E)-4-[(2,3-dihydro-2,2,4,4,- tetramethyl-2H-1-benzo-[b]thiopyran-6-Yl)-1-propenyl]-2-methylbenzoic acid
Subramanian, Shunkar,Smith, Chad M.,Tabatabai, Ali,Bryan, Clinton D.,Buettner, Brian,Hale, Steve,Wakefield, Cynthia A.,Benbrook, Doris M.,Berlin, K. Darrell
, p. 67 - 77 (2007/10/03)
The syntheses of ethyl (E)-4-[(2,3-dihydro-2,2,4,4-tetramethyl-2H-1- benzo[b]-thiopyran-6-yl)-1-propenyl]-2-methylbenzoate (1) and (E)-4- [(2,3-dihydro-2,2,4,4-tetramethyl-2H-1-benzo[b]thiopyran-6-yl)-1-pro- penyl]-2-methylbenzoic acid (2) have been achieved. In comparison to ester 1, acid 2 exhibited greater efficacy in activating RARα, RARβ, and RARγ as well as greater potency in activating RARα and RARβ. Interestingly, both the ester 1 and acid 2 exhibited nearly equal potency in activating RARγ. Both compounds also induced tissue transglutaminase (TGase) activity approximately 50% of the level induced by trans-retinoic acid. An X-ray diffraction analysis of (E)-2 revealed the aryl rings as nearly orthogonal [74.0(2)°] and a torsional angle of 46.5(2)° between the thiochroman group and the propenyl group. Conjugation between such groups may not be a stringent requirement for receptor activation. Copyright Taylor & Francis Inc.
Photochemistry of bicyclo[2.2.2]oct-7-ene-2,5-diones and the corresponding 5-hydroxyimino and 5-methylene derivatives
Yang, Ming-Shyong,Lu, Shyue-Sheng,Rao, Chitneni Prasad,Tsai, Yow-Fu,Liao, Chun-Chen
, p. 6543 - 6553 (2007/10/03)
Synthesis and photochemistry of several title compounds 1-3 containing multiple chromophoric systems are described. The Diels-Alder reactions of 2,6,6-trimethylcyclohexa-2,4-dienone (5) with acetylenes 6a-d provided the adducts 7a-d, which upon hydrolysis furnished the desired bicyclo[2.2.2]octenediones 1a-d. Oximes 2a-d were prepared from diones 1a-d by treatment with hydroxylamine hydrochloride in pyridine. 5-Methylenebicyclo[2.2.2]oct-7-en-2-ones 3a-d were obtained via chemoselective Wittig reaction of the corresponding diones 1a-d. Bicyclo[2.2.2]-octenediones 1a-c underwent chemoselective oxa-di-π-methane rearrangement under sensitized conditions and suffered formal ketene extrusion upon direct irradiation. Direct irradiation of ld afforded 11d via formal ketene extrusion but under sensitization it remained unchanged. Oximes 2a-d suffered ketene extrusion upon direct irradiation and E/Z isomerization under sensitized conditions. On the other hand, 5-methylenebicyclo[2.2.2]oct-7-en-2-ones 3a-d generally underwent 1,3-acyl shift. The plausible courses of all these photochemical processes are discussed.
