28145-35-9Relevant articles and documents
6,7-Dimethoxy-2-phenethyl-1,2,3,4-tetrahydroisoquinoline amides and corresponding ester isosteres as multidrug resistance reversers
Bartolucci, Gianluca,Braconi, Laura,Colabufo, Nicola Antonio,Contino, Marialessandra,Dei, Silvia,Giampietro, Roberta,Manetti, Dina,Perrone, Maria Grazia,Riganti, Chiara,Romanelli, Maria Novella,Teodori, Elisabetta,Chiaramonte, Niccolò
, p. 974 - 992 (2020/04/24)
Aiming to deepen the structure–activity relationships of the two P-glycoprotein (P-gp) modulators elacridar and tariquidar, a new series of amide and ester derivatives carrying a 6,7-dimethoxy-2-phenethyl-1,2,3,4-tetrahydroisoquinoline scaffold linked to different methoxy-substituted aryl moieties were synthesised. The obtained compounds were evaluated for their P-gp interaction profile and selectivity towards the two other ABC transporters, multidrug-resistance-associated protein-1 and breast cancer resistance protein, showing to be very active and selective versus P-gp. Two amide derivatives, displaying the best P-gp activity, were tested in co-administration with the antineoplastic drug doxorubicin in different cancer cell lines, showing a significant sensitising activity towards doxorubicin. The investigation on the chemical stability of the derivatives towards spontaneous or enzymatic hydrolysis, showed that amides are stable in both models while some ester compounds were hydrolysed in human plasma. This study allowed us to identify two chemosensitizers that behave as non-transported substrates and are characterised by different selectivity profiles.
Preparation method of p-(2-methoxyl)ethyl phenol
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, (2019/05/08)
The invention discloses a preparation method of p-(2-methoxyl) ethyl phenol. According to the preparation method, p-chlorophenol is taken as the raw material, after etherification reactions, p-chlorophenol with a protected phenolic hydroxyl group is obtained, and after Grignard reactions, chlorination reactions, and methoxyl substitution reactions, p-(2-methoxyl)ethyl phenol is generated. The provided preparation method has the advantages of easily available raw materials, mild reaction conditions, high safety coefficient, strong operability, simple technology, easy industrialization, high product purity, and stable quality. The prepared p-(2-methoxyl)ethyl phenol totally meets the using requirements of medical intermediates.
Phenol compound and preparation method
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Paragraph 0089-0092, (2018/04/27)
The invention relates to a phenol compound and a preparation method. In an organic solvent, aryl halide and oxygen or air are used as reaction raw materials, and under the combined facilitation effectof a copper catalyst, alkali and an additive, the aryl halide and the oxygen react in illumination of light to obtain the phenol compound. The copper catalyst and the alkali have key effects in a reaction process. The preparation method of the phenol compound has the advantages of wide substrate range, operation at room temperature, simple aftertreatment, high yield and purity of products and thelike. A new synthetic route and method are opened for the phenol compound, and thus, the phenol compound has good application potential and research value.