1669-85-8Relevant academic research and scientific papers
Ru-Catalyzed Switchable N-Hydroxyethylation and N-Acetonylation with Crude Glycerol
Xin, Zhuo,Jia, Le,Huang, Yuxing,Du, Chen-Xia,Li, Yuehui
, p. 2007 - 2011 (2020/03/19)
Highly efficient Ru-catalyzed selective C?C or C?O bond cleavage of polyols (e.g., crude glycerol) for N-hydroxyethylation or N-acetonylation of amines was achieved through the hydrogen-borrowing approach. A variety of amines were transformed to the desired amino alcohols/ketones in moderate-to-excellent yields, opening up new avenues for generation of oxygenated pharmaceuticals and fine chemicals from renewable raw materials. The use of new redox-active catalysts containing bisphosphine/thienylmethylamine ligands allows this hydrogen-borrowing system to be operated selectively under both basic and acidic conditions.
A 4 - (N - methyl - N - sulfo ethyl) amino formaldehyde sodium synthesis method
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Paragraph 0031-0050, (2018/06/19)
The present invention discloses a 4-(N-methyl-N-sulfoethyl)aminobenzaldehyde sodium salt synthesis method, which comprises: adding N-methyl-N-hydroxyethyl aniline and a chlorine-containing oxide to an organic solvent to carry out a substitution reaction so as to generate N-methyl-N-chloroethylaniline, carrying out a Vilsmeier-Haack reaction of the N-methyl-N-chloroethylaniline, disubstituted formamide and phosphorus oxychloride to generate N-methyl-N-chloroethyl-4-aminobenzaldehyde, and carrying out a sulfonation reaction of the N-methyl-N-chloroethyl-4-aminobenzaldehyde and a sulfonation agent in an alkaline solution to generate the 4-(N-methyl-N-sulfoethyl)aminobenzaldehyde sodium salt. The method of the present invention has characteristics of cheap and readily available raw materials and simple process, and is suitable for large-scale industrial production.
Novel ROS-activated agents utilize a tethered amine to selectively target acute myeloid leukemia
Bell-Horwath, Tiffany R.,Vadukoot, Anish K.,Thowfeik, Fathima Shazna,Li, Guorui,Wunderlich, Mark,Mulloy, James C.,Merino, Edward J.
supporting information, p. 2951 - 2954 (2013/06/27)
This study explores the possible use of reactive oxygen-activated DNA modifying agents against acute myeloid leukemia (AML). A key amine on the lead agent was investigated via cytotoxicity assays and was found necessary for potency. The two best compounds were screened via the NCI-60 cell panel. These two compounds had potency between 200 and 800 nM against many of the leukemia cancer cell types. Subsequent experiments explored activity against a transformed AML model that mimics the molecular signatures identified in primary AML patient samples. A lead compound had an IC50 of 760 nM against this AML cell line as well as a therapeutic index of 7.7 ± 3 between the transformed AML model cell line and non-cancerous human CD34+ blood stem/progenitor cells (UCB). The selectivity was much greater than the mainstays of AML treatment: doxorubicin and cytarabine. This manuscript demonstrates that this novel type of agent may be useful against AML.
ROS-Activated Compounds as Selective Anti-Cancer Therapeutics
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Paragraph 0123, (2013/09/12)
Provided are compounds according to the following Formula I: The Formula I compounds are activated in the presence of reactive oxygen species (ROS) and are therefore selective anti-cancer therapeutics for cancers associated with elevated ROS. Also provided are methods and pharmaceutical compositions for treating cancers associated with increased ROS.
Synthesis and pharmacological activity of some new pyridazinones
Corsano, S,Strappaghetti, G,Codagnone, A,Scapicchi, R,Marucci, G
, p. 545 - 549 (2007/10/02)
The synthesis of a series of piperazinyl-pyridazinones is reported. The blocking activity of these compounds was determined on the pre- and postsynaptic α-adrenoreceptors of isolated rat vas deferens. For compounds 7, 17 and 18, the hypotensive activity w
Aminopiperidines, their production and the pharmaceutical compositions incorporating them
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, (2008/06/13)
This invention relates to 4-aminopiperidines and more precisely to 4-aminopiperidines the nitrogen atom of the piperidine ring is substituted with an aryl lower alkyl side-chain. This invention also relates to processes for producing the same. This invention further extends to pharmaceutical compositions and to the method of using the same.
