37148-47-3Relevant articles and documents
Preparation method of stable isotope labeled clenproperol
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Paragraph 0041-0045, (2021/07/09)
The invention relates to a preparation method of stable isotope labeled clenproperol, which comprises the following steps: by taking 4-amino-3,5-dichloroacetophenone (II) as a raw material, carrying out bromination reaction to prepare a compound (III), then carrying out improved Gabriel synthesis reaction, namely amination reaction with sodium diformamide to obtain a compound (IV), then carrying out hydrolysis and reduction to obtain a compound (VI), and carrying out reductive amination reaction to generate a target compound (I). The preparation method disclosed by the invention is reasonable in process design, low in raw material price, controllable in experimental process and simple and convenient to operate, various required labeled compounds such as D-labeled, 13C-labeled or D/13C double-labeled compounds can be conveniently synthesized, and the prepared target product is high in purity, can be used as an internal standard substance in the field of food safety detection, and has important practical application value.
Red-shifted tetra-ortho-halo-azobenzenes for photo-regulated transmembrane anion transport
Bo, Zonghua,Duarte, Fernanda,Kerckhoffs, Aidan,Langton, Matthew J.,Penty, Samuel E.
, p. 9058 - 9067 (2021/11/04)
Photo-responsive synthetic ion transporters are of interest as tools for studying transmembrane transport processes and have potential applications as targeted therapeutics, due to the possibility of spatiotemporal control and wavelength-dependent function. Here we report the synthesis of novel symmetric and non-symmetric red-shifted tetra-ortho-chloro- and tetra-ortho-fluoro azobenzenes, bearing pendant amine functionality. Functionalisation of the photo-switchable scaffolds with squaramide hydrogen bond donors enabled the preparation of a family of anion receptors, which act as photo-regulated transmembrane chloride transporters in response to green or red light. The subtle effects of chlorine/fluorine substitution,meta/parapositioning of the anion receptors, and the use of more flexible linkers are explored. NMR titration experiments on the structurally diverse photo-switchable receptors reveal cooperative binding of chloride in theZ, but notEisomer, by the two squaramide binding sites. These results are supported by molecular dynamics simulations in explicit solvent and model membranes. We show that this intramolecular anion recognition leads to effective switching of transport activity in lipid bilayer membranes, in which optimalZisomer activity is achieved using a combination of fluorine substitution andpara-methylene spacer units.
Phenylethanolamine β receptor agonist synthetic method
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Paragraph 0038; 0042-0044, (2019/07/04)
The invention discloses a phenylethanolamine β receptor agonist synthetic method, comprises the following steps: S1: the 4 - amino acetophenone dissolved in an organic solvent, with the electrophilic reagent occurs on the benzene ring substituted halogenated reaction, generating [...] intermediate; [...] intermediates in organic solvent or in water, under the catalysis of the metal catalyst with the cyanide reagent undergo nucleophilic substitution reaction, generating phenyl ketone intermediate; S2: phenyl ketone intermediates in organic solvent, with the copper bromide generating carbonyl α bromo reaction to produce α - bromoacetophenone intermediates; S3: α - bromoacetophenone intermediates in organic solvent with tert-butyl amine or isopropylamine reaction intermediates acetophenone amines; S4: acetophenone amine intermediates in organic solvent, with the reduction hydrogenation reagent react to generate the phenylethanolamine β receptor agonists; synthetic method of this invention a simple and highly efficient and cheap and easy to obtain, atom utilization is high, the synthetic product chemical purity is greater than 99%, to meet the detection requirements of the food safety.