6956-85-0Relevant academic research and scientific papers
Synthesis and herbicidal activities of aryloxyacetic acid derivatives as HPPD inhibitors
Huang, Hao,Liu, Jian-Min,Shu, Lei,Wang, Man-Man,Yan, Yi-Le,Zhang, Da-Yong,Zhang, Jian-Qiu
supporting information, p. 233 - 247 (2020/03/27)
A series of aryloxyacetic acid derivatives were designed and synthesized as 4-hydoxyphenylpyruvate dioxygenase (HPPD) inhibitors. Preliminary bioassay results reveal that these derivatives are promising Arabidopsis thaliana HPPD (AtHPPD) inhibitors, in particular compounds I12 (Ki = 0.011 μM) and I23 (Ki = 0.012 μM), which exhibit similar activities to that of mesotrione, a commercial HPPD herbicide (Ki = 0.013 μM). Furthermore, the newly synthesized compounds show significant greenhouse herbicidal activities against tested weeds at dosages of 150 g ai/ha. In particular, II4 exhibited high herbicidal activity for pre-emergence treatment that was slightly better than that of mesotrione. In addition, compound II4 was safe for weed control in maize fields at a rate of 150 g ai/ha, and was identified as the most potent candidate for a novel HPPD inhibitor herbicide. The compounds described herein may provide useful guidance for the design of new HPPD inhibiting herbicides and their modification.
Design and Synthesis of Novel 4-Hydroxyl-3-(2-phenoxyacetyl)-pyran-2-one Derivatives for Use as Herbicides and Evaluation of Their Mode of Action
Lei, Kang,Li, Pan,Yang, Xue-Fang,Wang, Shi-Ben,Wang, Xue-Kun,Hua, Xue-Wen,Sun, Bin,Ji, Lu-Sha,Xu, Xiao-Hua
, p. 10489 - 10497 (2019/10/02)
In order to develop a novel herbicide containing the β-triketone motif, a series of 4-hydroxyl-3-(2-phenoxyacetyl)-pyran-2-one derivatives were designed and synthesized. The bioassay results showed that compound II15 had good pre-emergent herbicidal activity even at a dosage of 187.5 g ha-1. Moreover, compound II15 showed a broader spectrum of weed control when compared with a commercial herbicide 2,4-dichlorophenoxyacetic acid (2,4-D), and displayed good crop safety to Triticum aestivum L. and Zea mays Linn. when applied at 375 g ha-1 under pre-emergence conditions, which indicated its great potential as a herbicide. More importantly, studying the molecular mode of action of compound II15 revealed that the novel triketone structure is a proherbicide of its corresponding phenoxyacetic acid auxin herbicide, which has a herbicidal mechanism similar to that of 2,4-D. The present work indicates that the 4-hydroxyl-3-(2-phenoxyacetyl)-pyran-2-one motif may be a potential lead structure for further development of novel auxin-type herbicides.
Preparation method of chlorophenoxyacetic ester
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Paragraph 0058; 0060, (2019/01/08)
The invention provides a preparation method of chlorophenoxyacetic ester, wherein the preparation method comprises the following steps: A) carrying out reaction of glycolic acid and alcohol in tolueneto obtain glycolic ester; B) carrying out reaction of glycolic ester and metal alkoxide to obtain a metal salt of glycolic ester; and C) carrying out reaction of the metal salt of glycolic ester andchlorobenzene to obtain the chlorophenoxyacetic ester. The chlorophenoxyacetic ester is synthesized by condensation of chlorobenzene with the metal salt of glycolic ester, the use of chlorophenol withunpleasant odor is effectively avoided, the production of highly toxic dioxins is eliminated, and the product quality and the operating environment of the production site are greatly improved. Motherliquor containing effective ingredients cannot be produced, so the loss of effective ingredients is effectively avoided and the yield of the product is improved.
Aza-Michael addition of acrylonitrile with 2-aryloxymethylbenzimidazole derivatives under microwave irradiation
Wei, Tai-Bao,Hua, Mao-Tang,Shi, Hai-Xiong,Liu, Yong,Zhang, You-Ming
scheme or table, p. 452 - 454 (2010/12/24)
A simple, rapid, and highly efficient method has been developed for the aza-Michael addition of acrylonitrile to 2-aryl-oxymethylbenzimidazole derivatives in the presence of anhydrous potassium carbonate under microwave irradiation. A series novel of 1-cyanoethyl-2-aryloxymethylbenzimidazole derivatives have been prepared and characterised by 1H NMR, 13C NMR, IR spectra and elemental analysis.
A rapid and high-yield synthesis of aryloxyacetyl hydrazides under microwave irradiation and with phase transfer catalysis
Wei, Tai-Bao,Liu, Hong,Li, Man-Lin,Zhang, You-Ming
, p. 432 - 433 (2007/10/03)
A series of aryloxyacetyl hydrazides 4a-l were synthesised under microwave irradiation and phase transfer catalysis conditions. By the optimisation of the reaction conditions, a rapid, high-yield and efficient method for the preparation of aryloxyacety hydrazide was given.
ISOQUINOLINE-5-SULFONIC ACID AMIDES AS INHIBITORS OF AKT (PROTEIN KINASE B)
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Page 18, (2010/02/09)
The present invention relates to compounds Formula (I): as inhibitors of AKT activity, which are useful for the treatment of susceptible neoplasms and viral infections.
Biological monitoring of 2,4,5-trichlorophenol (I): preparation of antibodies and development of an immunoassay using theoretical models.
Nichkova, Mikaela,Galve, Roger,Marco, M-Pilar
, p. 1360 - 1370 (2007/10/03)
Antibodies against 2,4,5-trichlorophenol have been prepared after theoretical and molecular modeling chemical studies of three potential immunizing haptens with the aim to find out the one mimicking best the target analyte. Competitive direct and indirect ELISAs have been developed after screening a battery of haptenized enzyme tracers and coating antigens, respectively. The relation between the degree of heterology of the competitor and the resulting immunoassay detectability has been investigated according to the electronic similarities of the competitor haptens with the target analyte taking in consideration their pK(a) values. These studies have been performed using theoretical and molecular modeling tools to find out their electronic distribution at their minimum energetic levels. The results suggest that the competitors should have a high homology to produced assays with good detectability values. On the other hand detectability improves when lowering the hapten density of the competitors. An indirect competitive ELISA has been finally selected for further investigation. The immunoassay has an IC(50) value of 0.6 microg L(-)(1) and a limit of detection of 0.084 microg L(-)(1). The selectivity of the assay is high in relation to other chlorophenols frequently present in real samples. In contrast, the brominated analogues may also be recognized with this assay.
C-amidoalkylation of the esters of aroxy- and arylthioacetic acids with trichloroethylidenarenesulfonamides
Levkovskaya,Krivonos,Rozentsveig,Mirskova,Albanov
, p. 240 - 244 (2007/10/03)
Esters of aroxyacetic and arylthioacetic acids react with chloral arenesulfonylimines in the presence of oleum affording in good yields the products of C-arenesulfonylamidoalkylation of the aromatic ring in 4 position.
Applicability of Hammett Equation to Kinetics of Acid-catalysed Esterification of ortho-Substituted Phenoxyacetic, Phenylmercaptoacetic and Phenylsulphonylacetic Acids by Methanol
Baliah, V.,Gurumurthy, R.
, p. 257 - 258 (2007/10/02)
Correlation analysis of the title rate data shows that the steric effects of ortho-substituents are absent at the reaction centre.
Applicability of Hammett Equation to Insulated Systems - Kinetics of Alkaline Hydrolysis of ortho-Substituted Methyl Phenoxyacetates
Gurumurthy, R.,Balakrishnan, N.
, p. 1114 - 1115 (2007/10/02)
Kinetics of alkaline hydrolysis of some ortho-substituted methyl phenoxyacetates in methanol-water (85percent wt/wt) at 10 deg, 15 deg and 20 deg are reported.The application of Taft's steric energy relationship shows that the reaction is not susceptible
