24938-60-1Relevant articles and documents
Design, synthesis, and mechanistic investigations of phenylalanine derivatives containing a benzothiazole moiety as HIV-1 capsid inhibitors with improved metabolic stability
Cherukupalli, Srinivasulu,Cocklin, Simon,De Clercq, Erik,Dick, Alexej,Ding, Dang,Ding, Xiao,Gao, Shenghua,Huang, Tianguang,Jiang, Xiangyi,Kang, Dongwei,Liu, Xinyong,Meuser, Megan E.,Pannecouque, Christophe,Sun, Lin,Tao, Yucen,Xu, Shujing,Zalloum, Waleed A.,Zhan, Peng,Zhang, Xujie
, (2021/10/14)
Further clinical development of PF74, a lead compound targeting HIV-1 capsid, is impeded by low antiviral activity and inferior metabolic stability. By modifying the benzene (region I) and indole of PF74, we identified two potent compounds (7m and 7u) wit
Synthesis of polyaramids in γ-valerolactone-based organic electrolyte solutions
Winters, Jonas,Bolia, Raheed,Dehaen, Wim,Binnemans, Koen
, p. 1228 - 1239 (2021/02/26)
The current synthetic procedures for polyaramids mainly involve the use of amide solvents such asN-methylpyrrolidone andN,N-dimethylacetamide. However, these solvents are suspected to be teratogenic and are considered ‘Substances of Very High Concern’ by the European Commission. Here we propose a benign alternative solvent system: an Organic Electrolyte Solution (OES) consisting of γ-valerolactone (GVL) and a small amount of the ionic liquid 1-methyl-3-octylimidazolium chloride, [C8MIm][Cl]. Three commercially relevant polyaramids were synthesized: poly-p-phenylene terephthalamide (PPTA), poly-m-phenylene isophthalamide (PMIA) and copoly(p-phenylene/3,4′-diphenylether terephthalamide) (ODA/PPTA). PMIA was successfully synthesized in the OES containing [C8MIm][Cl] in a molar fraction ofxIL= 0.043, achieving an inherent viscosity ofηinh= 1.94 ± 0.064 dL g?1, which is on par with the current industrial standard and the benchmark lab scale synthesis. The reaction mixture could also be directly used for the wet spinning of polyaramid fibers, and all components of the solvent could be recycled in good yields by a series of evaporation and distillation steps. ODA/PPTA could be synthesized, but only rather low inherent viscosities were achieved. The reaction mixture was too viscoelastic to be spun by our small-scale spinning setup. PPTA always instantly precipitated and could not be synthesized from a [C8MIm][Cl]/GVL OES. α-Picoline, the organic base which was added to capture the released HCl during the reaction, was found to play a pivotal role in the polymerization reaction. By undergoing an acid-base reaction with HCl, it forms a protic ionic liquidin situwhich increases the solubility of the polymer.
Meta-Substituted benzamide oligomers that complex mono-, di- and tricarboxylates: Folding-induced selectivity and chirality
Shi, Zhu-Ming,Chen, Shi-Gui,Zhao, Xin,Jiang, Xi-Kui,Li, Zhan-Ting
experimental part, p. 8122 - 8129 (2012/01/04)
meta-Substituted arylamide trimer, pentamer and heptamer have been prepared from simple benzene-1,3-diamine, benzene-1,3-dicarboxylic acid, and 3-aminobenzoic acid units. 2D NOESY 1H NMR experiments reveal that these flexible oligomers form fol
