2948-16-5Relevant academic research and scientific papers
Synthesis method of noradrenaline impurity
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Paragraph 0009-0012, (2021/07/01)
The invention discloses a synthesis method of a noradrenaline impurity. The impurity is 2-chloro-2', 3'-dihydroxyacetophenone, which belongs to the field of drug synthesis by taking catechol as an initial raw material through two-step reaction. The most e
Synthesis and biological evaluation of phenstatin metabolites
Ghinet, Alina,Rigo, Beno?t,Hénichart, Jean-Pierre,Le Broc-Ryckewaert, Delphine,Pommery, Jean,Pommery, Nicole,Thuru, Xavier,Quesnel, Bruno,Gautret, Philippe
, p. 6042 - 6054 (2011/11/29)
Previous investigations on the incubation of phenstatin with rat and human microsomal fractions revealed the formation of nine main metabolites. The structures of eight of these metabolites have been now confirmed by synthesis and their biological properties have been reported. Eaton's reagent was utilized as a convenient condensing agent, allowing, among others, a simple multigram scale preparation of phenstatin. Synthesized metabolites and related compounds were evaluated for their antiproliferative activity in the NCI-60 cancer cell line panel, and for their effect on microtubule assembly. Metabolite 23 (2′-methoxyphenstatin) exhibited the most potent in vitro cytotoxic activity: inhibition of the growth of K-562, NCI-H322M, NCI-H522, KM12, M14, MDA-MB-435, NCI/ADR-RES, and HS 578T cell lines with GI50 values 50 = 3.2 μM vs 15.0 μM) and induced G2/M arrest in murine leukemia DA1-3b cells. The identification of this active metabolite led to the design and synthesis of analogs with potent in vitro cytotoxicity and inhibition of microtubule assembly.
Microwave-assisted synthesis of aromatic bis-esters in liquid phase
Zbancioc, Gheorghita N.,Zbancioc, Ana Maria V.,Mangalagiu, Ionel I.
experimental part, p. 117 - 122 (2011/08/05)
A fast, general, environmentally friendly, and facile method for preparation of phenyl bis-esters under microwave irradiation in liquid phase is presented. Selective reaction pathways in order to get phenyl bis-esters only or phenyl monoesters only have b
Hydroxyphenyl- and hydroxyphenoxyalkanoic acid iodopropargyl esters
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, (2008/06/13)
The invention concerns compounds having the formula STR1 wherein R1, R2, R3, R4 can mean identical or different radicals in any desired position on the benzene ring, namely fluoro, chloro, bromo, iodo, cyano, or
