17583-00-5Relevant articles and documents
Substituted conformationally restricted guanidine derivatives: Probing the α2-adrenoceptors’ binding pocket
McMullan, Michela,García-Bea, Aintzane,Miranda-Azpiazu, Patricia,Callado, Luis F.,Rozas, Isabel
, p. 48 - 57 (2016)
In this paper we report the design, synthesis and pharmacological evaluation of new N-substituted 2-amino-1,4-dihydroquinazolines, 2-amino-1,4-dihydropyridopyrimidines and 2-amino-4,5-dihydro-1,3-benzodiazepines as α2-adrenoceptors ligands. Computational studies show that the proposed substitutions and guanidine-containing ring size will probe an extensive area of the active site. Preparation of these molecules involved novel routes than those previously utilised in our laboratory for the preparation of the acyclic aryl-guanidine counterparts. Compounds 8b and 18c showed the highest affinity and antagonistic activity, within their series, towards the α2-adrenoceptor in human brain tissue in?vitro experiments. Structure-activity relationships have been established for the design and biological evaluation of novel α2-adrenoceptor ligands.
Synthesis method of N-phenyl aminobenzoic acid
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Paragraph 0007; 0027-0030; 0033-0036; 0039-0042; 0045-0047, (2021/01/11)
The invention belongs to the technical field of organic intermediate synthesis, and particularly relates to a synthesis method of N-phenyl aminobenzoic acid. The method comprises the following steps:(1) dissolving 2-chlorobenzonitrile and aniline in a solvent, adding K2CO3 and NaOH while stirring, and heating to carry out primary reflux reaction; (2) after the reflux reaction is finished, recovering the solvent under reduced pressure, then cooling the residual liquid, adding water, and heating to carry out secondary reflux reaction; and (3) cooling the reaction solution after the secondary reflux reaction in the step (2) to room temperature, extracting excessive aniline, adding diluted hydrochloric acid for neutralization while stirring a water phase, separating out a solid, filtering, and recrystallizing to obtain the target product N-phenyl aminobenzoic acid. According to the method, a one-pot process is adopted, under the condition that a catalyst is not used, 2-chlorobenzonitrileand aniline are used as raw materials for reaction, the target product with high purity (larger than 99%) and high yield (larger than 90%) is obtained, operation is easy, the raw materials are easy toobtain, the reaction is mild and easy to control, and aftertreatment is simple.
COMPOUND FOR ORGANIC ELECTRONIC ELEMENT, ORGANIC ELECTRONIC ELEMENT USING THE SAME, AND AN ELECTRONIC DEVICE THEREOF
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Paragraph 0335; 0437-0443, (2020/08/28)
The present invention relates to a device for emitting light. Provided are a novel mixture capable of improving stability and longevity, an organic electronic element using the same, and an electronic device thereof. (by machine translation)
