4084-38-2Relevant academic research and scientific papers
The Pyrethrins and Related Compounds. Part XL - Structure-Activity Relationships of Pyrethroidal Esters with Acyclic Side Chains in the Alcohol Component against Resistant Strains of Housefly (Musca domestica)
Farnham, Andrew W.,Khambay, Bhupinder P. S.
, p. 277 - 282 (1995)
Activities of a range of pyrethroidal esters, incorporating structural variations in all regions of the acid and alcohol components, have been measured against two fully characterised and homozygous resistant strains of Musca domestica L. (kdr and super-kdr). The results, limited in this paper to esters of alcohols with acyclic side chains, show the same level of uniform resistance to the kdr strain observed previously, across a range of acid and alcohol variations. Against the super-kdr strain, in contrast to the cyclic side chain set, resistance factors are barely higher than for the kdr strain. Against super-kdr flies, some dependence of resistance factor on the position of the side chain substituent was detected. Polyfluorobenzyl esters confer particularly low resistance factors.
Synthetic method of transfluthrin intermediate
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Paragraph 0047; 0055-0056; 0057; 0065-0066; 0067; ..., (2021/08/25)
The invention discloses a synthetic method of a transfluthrin intermediate, and belongs to the technical field of chemical synthesis, the synthetic method is characterized by comprising the following steps: (1) taking 2, 3, 5, 6-tetrafluorobenzene as a raw material, and reacting with carbon tetrachloride to obtain 2, 3, 5, 6-tetrafluorotrichloromethyl benzene; (2) under the action of a composite catalyst, carrying out catalytic hydrolysis on the 2, 3, 5, 6-tetrafluorotrichloromethyl benzene to obtain 2, 3, 5, 6-tetrafluorobenzoyl chloride; (3) under the action of a catalyst, the 2, 3, 5, 6-tetrafluorobenzoyl chloride and hydrogen are subjected to a Rosenmonde reduction reaction, and 2, 3, 5, 6-tetrafluorobenzaldehyde is obtained; (4) carrying out catalytic hydrogenation reaction on the 2, 3, 5, 6-tetrafluorobenzaldehyde and hydrogen to obtain 2, 3, 5, 6-tetrafluorobenzyl alcohol; the method has the advantages of simple steps, high yield of each step and simple reaction; the reaction conditions of each step are mild, and the method has the advantages of low cost, high yield and easily available reaction conditions.
Direct evidence of edge-to-face CH/π interaction for PAR-1 thrombin receptor activation
Asai, Daisuke,Inoue, Naoko,Sugiyama, Makiko,Fujita, Tsugumi,Matsuyama, Yutaka,Liu, Xiaohui,Matsushima, Ayami,Nose, Takeru,Costa, Tommaso,Shimohigashi, Yasuyuki
, (2021/11/20)
Heptapeptide SFLLRNP is a receptor–tethered ligand of protease-activated receptor 1 (PAR-1), and its Phe at position 2 is essential for the aggregation of human platelets. To validate the structural elements of the Phe-phenyl group in receptor activation, we have synthesized a complete set of S/Phe/LLRNP peptides comprising different series of fluorophenylalanine isomers (Fn)Phe, where n = 1, 2, 3, and 5. Phe-2-phenyl was strongly suggested to be involved in the edge-to-face CH/π interaction with the receptor aromatic group. In the present study, to prove this receptor interaction definitively, we synthesized another series of peptide analogs containing (F4)Phe-isomers, with the phenyl group of each isomer possessing only one hydrogen atom at the ortho, meta, or para position. When the peptides were assayed for their platelet aggregation activity, S/(2,3,4,6-F4)Phe/LLRNP and S/(2,3,4,5-F4)Phe/LLRNP exhibited noticeable activity (34% and 6% intensities of the native peptide, respectively), whereas S/(2,3,5,6-F4)Phe/LLRNP was completely inactive. The results indicated that, at the ortho and meta positions but not at the para position, benzene-hydrogen atoms are required for the CH/π interaction to activate the receptor. The results provided a decisive evidence of the molecular recognition property of Phe, the phenyl benzene-hydrogen atom of which participates directly in the interaction with the receptor aromatic π plane.
A substituted aromatic alcohols of the economical efficiency of the synthesis process (by machine translation)
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Paragraph 0029; 0033; 0034; 0037; 0038; 0042, (2019/05/15)
The invention discloses a substituted aromatic alcohols of the economical efficiency of the synthesis process, the COOR1 - C6 F4 - COOR1 (R1 Representative C1 - C4 Alkyl) to the organic solvent in the input, in the NaBH4 Under the action of the shall CH reduction reaction2 OH - C6 F4 - CH2 OH (II) and CH2 OH - C6 F4 - COOH (III); the mixture is dissolved in a weak acid buffer solution, after adjusting the pH of the extraction, the aqueous layer containing in II, III contained in the oil reservoir; the oil reservoir into the non-protic solvent removes the carboxyl, shall be CH2 OH - C6 HF4 . The present invention, reduction process residence in the intermediate state, the process on the reduction reducing the requirements of the complete degree, reduce the used as the reducing agent; the mixture with chemical separation, the product is very good use can be obtained. (by machine translation)
Preparation method of tetrafluorobenzene methanol
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Paragraph 0035; 0037-0046, (2019/02/13)
Belonging to the technical field of organic synthesis, the invention discloses a preparation method of tetrafluorobenzene methanol. The method includes: reacting tetrafluorobenzoic acid with thionyl chloride to produce tetrafluorobenzoyl chloride, then taking tetrafluorobenzoyl chloride as the raw material, and conducting reduction in water with sodium borohydride activated by an ether solvent toobtain tetrafluorobenzene methanol. According to the invention, the ether solvent and sodium borohydride are subjected to complexing to activate sodium borohydride, water is adopted as the solvent forreduction, the reaction yield is high, the reductant sodium borohydride can complete the reaction at a catalytic amount, and the reaction process is greener and more environmentally friendly.
Tetrafluorobenzyl alcohol producing mechanical device
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Paragraph 0011; 0012; 0013, (2017/06/23)
The present invention discloses a tetrafluorobenzyl alcohol producing mechanical device and belongs to the machinery field of fine chemical engineering production. The mechanical device comprises: a chemical reacting kettle (1), a decolorizing kettle (2), a distilling kettle (3), and a dryer (4). The mechanical device is characterized in that a 2,3,5,6-tetrafluoro-benzoic acid inlet (5), an ethylene glycol dimethyl ether inlet (6), an ethylene glycol dimethyl ether solution inlet of sodium borohydride (7), and an ethylene glycol dimethyl ether solution inlet of sulfate dimethyl ether (8). A first material pulp pump and a pipeline (9) are arranged between the chemical reacting kettle (1) and the decolorizing kettle (2). An activated carbon inlet (10) is arranged on the decolorizing kettle (2). A second material pulp pump and a pipeline (11) are arranged between the decolorizing kettle (2) and the distilling kettle (3). A steam outlet (12) is arranged on distilling kettle (3). A second conveyor (13) is arranged between the distilling kettle (3) and the dryer (4). A finished product outlet (14) is arranged on the dryer (4).
Mg-Prompted Polyfluoroarene C-H Functionalization: Formal Synthesis of Transfluthrin, Fenfluthrin, and Tefluthrin
Jia, Xuejiao,Wang, Junya,Ding, Xue,Yang, Jun,Li, Nan,Zhao, Na,Huang, Zhiyan
, p. 10874 - 10882 (2015/11/18)
Directing group and transition metal free C-H bond functionalization of a simple molecule is an ideal but challenging chemical transformation. Herein, we report a general Mg-prompted approach to synthesize versatile polyfluoroaryl carbinols at ambient temperature via polyfluoroarene C-H bond addition to aldehydes, which featured excellent monoaddition selectivity and broad functional group compatibility. The usefulness of this practical and efficient method was demonstrated in gram-scale formal synthesis of pyrethroid insecticides transfluthrin, tefluthrin, and fenfluthrin.
A new synthetic route to polyfluorobenzyl alcohol
Zhang, Deyan,Chen, Zizhan,Cai, Huihua,Zou, Xinzhuo
experimental part, p. 938 - 941 (2010/01/15)
The synthesis of polyfluorinated benzyl alcohol from pentafluorobenzoic acid has been developed. An economical and effective direct reduction method of polyfluorobenzoic acid by zinc borohydride is described.
Process for producing tetrafluorobenzenemethanols
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, (2008/06/13)
The present invention relates to a process by a series of reactions using tetrafluorocyanobenzens as material for producing tetrafluorobenzenemethanols, tetrafluorobenzenecarbaldehyde dialkylacetals and tetrafluorobenzenecarbaldehydes in a high purity and a high yield which are useful as intermediates in the production of cyclopropanecarboxylic acid esters having insecticidal action, and also relates to a novel tetrafluorobenzenecarbaldehyde dimethylacetal.
Process for producing cyclopropanecarboxylates
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, (2008/06/13)
There is disclosed a process process for producing a cyclopropanecarboxylate of formula (1): 1which process comprises reacting cyclopropanecarboxylic acid of formula (2): 2with a monohydroxy compound of formula (3): R6OH??(3),in the presence of a catalyst compound comprising an element of to Group 4 of the Periodic Table of Elements.
