6232-88-8Relevant academic research and scientific papers
Extended peptoids: a new class of oligomers based on aromatic building blocks
Combs, David J.,Lokey, R. Scott
, p. 2679 - 2682 (2007)
Peptoids (N-substituted polyglycines) represent a class of bioinspired oligomers that have unique physical and structural properties. Here, we report the construction of 'extended peptoids' based on aromatic building blocks, in which the N-alkylaminoacetyl group of the peptoid backbone has been replaced by an N-alkylaminomethylbenzoyl spacer. Both meta- and para-bromomethylbenzoic acids were synthesized, providing access to a new class of peptoids. Further, inclusion of hydrophilic side chains confers water solubility to these compounds, showing that, like simple peptoids, extended peptoids add an extra dimension to synthetic poly-amide oligomers with potential application in a variety of biological contexts.
P-aminomethyl benzoic acid and preparation method thereof
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Paragraph 0020; 0033-0034; 0038-0040; 0044-0046; 0049, (2020/09/09)
The invention discloses p-aminomethyl benzoic acid and a preparation method thereof. The method comprises the following steps: hydrolyzing phthalic anhydride as a raw material under an alkaline condition to enable the anhydride structure of phthalic anhydride to be subjected to ring opening to obtain an intermediate 1; performing decarboxylation reaction on the intermediate 1 under the condition that high-temperature liquid water is used as a reaction medium to obtain an intermediate 2; converting original binary acid of the intermediate 1 into monobasic acid, and enabling the intermediate 2 to react with a saturated monochloromethane diethyl ether solution by taking diethyl ether as a solvent under the catalytic action of aluminum chloride to obtain an intermediates 3; and carrying out bromine substitution reaction on the intermediate 3 and N-bromosuccinimide, and carrying out ammoniation reaction under the action of triethylamine and potassium carbonate. The yield of p-aminomethyl benzoic acid prepared by the preparation method of p-aminomethyl benzoic acid is high, and compared with an existing preparation method, most of the used raw materials are low-price raw materials, cyanogroups with high toxicity are not introduced, and the production cost of tranexamic acid is greatly reduced.
Photoinduced Carbon Tetrabromide Initiated Aerobic Oxidation of Substituted Toluenes to Carboxylic Acids
Li, Xiaoqing,Xu, Xiangsheng,Yan, Xiaoyu,Yan, Xinhuan,Zhang, Guofu,Zheng, Kun
, p. 272 - 274 (2020/02/18)
A mild and metal-free procedure is reported for the aerobic oxidation of substituted toluenes to carboxylic acids by using CBr 4 as initiator under irradiation from a 400 nm blue light-emitting diode.
INHIBITORS OF PSEUDOMONAS AERUGINOSA VIRULENCE
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Paragraph 0125, (2019/04/16)
Disclosed are piperazine derivative compounds, particularly piperazine derivative compounds having a structure of Formula (I) and methods for preparing these compounds. Also disclosed are use of a therapeutically effective amount of the compound of Formula (I) or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition therefore for inhibiting quorum sensing of a bacteria.
Synthesis method of benzoic acid compounds
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Paragraph 0170; 0171; 0172; 0173, (2019/12/25)
The invention discloses a photocatalytic oxidation synthesis method of benzoic acid compounds, and the photocatalytic oxidation synthesis method comprises the following specific steps: mixing and dissolving toluene compounds and a catalyst in a solvent, reacting for 24-60h in the presence of an oxidant under the conditions of 350-460 nm LED illumination and a temperature of 20-80 DEG C, and performing post-treatment on the reaction liquid to obtain the benzoic acid compounds. The photocatalytic oxidation synthesis method has the advantages of no need of metal catalysts, simple operation and mild reaction conditions; oxygen is used as an oxidant, and the photocatalytic oxidation synthesis method has high atom economy, cheap reagent and environmental protection. The photocatalytic oxidationsynthesis method has good substrate applicability, and various substituents can realize the synthesis of corresponding benzoic acid compounds.
Split-and-Combine Approach Towards Branched Precision Glycomacromolecules and Their Lectin Binding Behavior
Baier, Mischa,Giesler, Markus,Hartmann, Laura
, p. 1619 - 1630 (2018/01/11)
Previously, monodisperse and sequence-controlled oligo(amidoamine) scaffolds were synthesized based on the step-wise assembly of tailor-made building blocks on a solid support that allow for the multivalent presentation of sugar ligands. Here, we extend on this concept using a split-and-combine approach to gain access to a small library of linear and branched glycomacromolecules. Azide side chains were introduced in the scaffold by the use of a novel building block allowing for copper-mediated azide-alkyne cycloaddition (CuAAC) of readily available propargyl-functionalized glycans. In the first stage, after assembly of the linear scaffold on solid support, the batch was divided into two. One part of the resin-bound oligomers was end-capped and further used as backbone and the other part was functionalized with propargylated α-d-mannopyranoside in the sidechain, end capped with an alkyne functionality and finally cleaved from solid support to give the branching arm. In the second stage, the linear, glycosylated and alkynylated arms were then coupled to the end capped backbone via CuAAC. In this way, branched glycomacromolecules with two and three branches, respectively, have been synthesized carrying from two to six sugar residues per molecule. Both, linear arms and branched glycomacromolecules were then subjected to a lectin binding assay using surface plasmon resonance (SPR) and model lectin Concanavalin A (Con A) showing the effect of branching as well as valency on the binding kinetics.
1. 3 - Benzoxazine - 2, 4 (3 H) - dione derivatives and their synthesis and use (by machine translation)
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Paragraph 0020; 0024; 0025, (2018/10/19)
The invention relates to a acetylcholine esterase with phosphodiesterase V enzyme inhibition benzoxazine dione derivative and its synthetic method and use, and in particular relates to the structure of the general formula (I) of 1, 3 benzoxazine - 2, 4 (3 H) - dione derivatives, R1 , R2 , R3 , R4 , R5 , R6 , R7 , R8 And R9 The specification of the existing limited to. This invention refers to these compound structure and synthetic method and in vitro acetylcholine esterase with phosphodiesterase V inhibiting activity, can be further developed into new drugs for treating Alzheimer's disease. (by machine translation)
[...] aromatic amines acetylcholine esterase inhibitor synthesis and use (by machine translation)
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Paragraph 0046; 0047; 0048, (2018/10/19)
The present invention provides a formula for the (I) or (II) [...] aromatic amines of the acetylcholine esterase inhibitor and its pharmaceutically acceptable salt or a stereoisomer thereof, a process for their preparation and its in the preparation of acetylcholine esterase inhibitors and treatment of Alzheimer's disease and/or myasthenic application of the medicament, type definition of each group in the specification. The invention of aromatic amine derivatives as [...] of acetylcholine esterase inhibitors with micromolar level to nanomolar inhibiting activity, has further developed into an anti-Alzheimer's disease possibility of drug. (by machine translation)
Tribromoisocyanuric acid as a green reagent for benzylic bromination of alkylarenes
De Almeida, Leonardo S.,Esteves, Pierre M.,De Mattos, Marcio C.S.
, p. 6843 - 6845 (2015/11/27)
The reaction of diverse alkylarenes with tribromoisocyanuric acid (0.34 mol equiv) in reflux EtOAc in the absence of any catalysts or light irradiation produced the corresponding benzyl bromides in 53-88% yield.
Controlling the Spatial Organization of Liquid Crystalline Nanoparticles by Composition of the Organic Grafting Layer
W?jcik, Micha? M.,Olesińska, Magdalena,Sawczyk, Micha?,Mieczkowski, J?zef,G?recka, Ewa
, p. 10082 - 10088 (2015/07/07)
Understanding how the spatial ordering of liquid crystalline nanoparticles can be controlled by different factors is of great importance in the further development of their photonic applications. In this paper, we report a new key parameter to control the mesogenic behavior of gold nanoparticles modified by rodlike thiols. An efficient method to control the spatial arrangement of hybrid nanoparticles in a condensed state is developed by changing the composition of the mesogenic grafting layer on the surface of the nanoparticles. The composition can be tuned by different conditions of the ligand exchange reaction. The thermal and optical behavior of the mesogenic and promesogenic ligands were investigated by using differential scanning calorimetry (DSC) and hot-stage polarized optical microscopy. The chemical structure of the synthesized hybrid nanoparticles was characterized by 1HNMR spectroscopy, thermogravimetric analysis (TGA), XPS, and elemental analysis, whereas the superstructures were examined by small-angle X-ray diffraction (SAXSRD) analysis. Structural studies showed that the organic sublayer made of mesogenic ligands is denser with an increasing the average ligand number, thereby separating the nanoparticles in the liquid crystalline phases, which changes the parameters of these phases. Softening nanocrystalline gold: An efficient method to control the spatial arrangement of liquid crystalline gold nanoparticles was developed by changing the composition of the mesogenic grafting layer. Structural studies showed that the organic sublayer is more dense with increasing average ligand number, thereby separating the nanoparticles in the liquid crystalline phases, which changes the parameters of these phases (see figure).
