94291-61-9Relevant articles and documents
From Anilines to Aryl Ethers: A Facile, Efficient, and Versatile Synthetic Method Employing Mild Conditions
Wang, Dong-Yu,Yang, Ze-Kun,Wang, Chao,Zhang, Ao,Uchiyama, Masanobu
, p. 3641 - 3645 (2018/03/13)
We have developed a simple and direct method for the synthesis of aryl ethers by reacting alcohols/phenols (ROH) with aryl ammonium salts (ArNMe3+), which are readily prepared from anilines (ArNR′2, R′=H or Me). This reaction proceeds smoothly and rapidly (within a few hours) at room temperature in the presence of a commercially available base, such as KOtBu or KHMDS, and has a broad substrate scope with respect to both ROH and ArNR′2. It is scalable and compatible with a wide range of functional groups.
Preparing method for efficient hexamidine dihydroxyethyl sulfonate
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Paragraph 0027; 0028; 0029, (2018/02/04)
The invention relates to a preparing method for efficient hexamidine dihydroxyethyl sulfonate. The preparing method is characterized by including the following steps that 1, sodium hydroxide and water are added into an ethanol solution of 4-cyanophenol, after reflux is carried out for 1 h, 1,6-dibromohexane is added, the mixture reacts for 3 h, and the product is filtered and dried to obtain 4,4'-dicyano-1,6-diphenoxy hexane; 2, anhydrous HCl gas is introduced into the product obtained in the previous step and reacts for 72 h at the temperature of 25 DEG C after gas introduction is completed, the product is filtered and dried to obtain 4,4'-imino ethyl ester-1,6-diphenoxy hexane; 3, dry ammonia gas is introduced into the product obtained in the previous step, reaction is carried out at controlled temperature for 15 h, then heating reflux is carried out for 9 h, isethionic acid is added, and a residue is heated to be dissolved, filtered in a suction mode while hot and dried to obtain hexamidine dihydroxyethyl sulfonate. It is found that the reaction has the advantages of being mild in condition, high in conversion rate and short in reaction time and has higher industrialized application value compared with prior synthesis methods.
Small Molecule Inhibitors of Ca2+-S100B Reveal Two Protein Conformations
Cavalier, Michael C.,Ansari, Mohd. Imran,Pierce, Adam D.,Wilder, Paul T.,McKnight, Laura E.,Raman, E. Prabhu,Neau, David B.,Bezawada, Padmavani,Alasady, Milad J.,Charpentier, Thomas H.,Varney, Kristen M.,Toth, Eric A.,MacKerell, Alexander D.,Coop, Andrew,Weber, David J.
, p. 592 - 608 (2016/02/09)
The drug pentamidine inhibits calcium-dependent complex formation with p53 (CaS100B·p53) in malignant melanoma (MM) and restores p53 tumor suppressor activity in vivo. However, off-target effects associated with this drug were problematic in MM patients. Structure-activity relationship (SAR) studies were therefore completed here with 23 pentamidine analogues, and X-ray structures of CaS100B·inhibitor complexes revealed that the C-terminus of S100B adopts two different conformations, with location of Phe87 and Phe88 being the distinguishing feature and termed the "FF-gate". For symmetric pentamidine analogues (CaS100B·5a, CaS100B·6b) a channel between sites 1 and 2 on S100B was occluded by residue Phe88, but for an asymmetric pentamidine analogue (CaS100B·17), this same channel was open. The CaS100B·17 structure illustrates, for the first time, a pentamidine analog capable of binding the "open" form of the "FF-gate" and provides a means to block all three "hot spots" on CaS100B, which will impact next generation CaS100B·p53 inhibitor design.
