4084-38-2Relevant articles and documents
Hecht
, p. 3503 (1968)
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)
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).
