- Ru-Catalyzed Switchable N-Hydroxyethylation and N-Acetonylation with Crude Glycerol
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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.
- Xin, Zhuo,Jia, Le,Huang, Yuxing,Du, Chen-Xia,Li, Yuehui
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p. 2007 - 2011
(2020/03/19)
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- A 4 - (N - methyl - N - sulfo ethyl) amino formaldehyde sodium synthesis method
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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.
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Paragraph 0031-0050
(2018/06/19)
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- Novel ROS-activated agents utilize a tethered amine to selectively target acute myeloid leukemia
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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.
- Bell-Horwath, Tiffany R.,Vadukoot, Anish K.,Thowfeik, Fathima Shazna,Li, Guorui,Wunderlich, Mark,Mulloy, James C.,Merino, Edward J.
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supporting information
p. 2951 - 2954
(2013/06/27)
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- ROS-Activated Compounds as Selective Anti-Cancer Therapeutics
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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.
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Paragraph 0123
(2013/09/12)
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- Synthesis and pharmacological activity of some new pyridazinones
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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
- Corsano, S,Strappaghetti, G,Codagnone, A,Scapicchi, R,Marucci, G
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p. 545 - 549
(2007/10/02)
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- Aminopiperidines, their production and the pharmaceutical compositions incorporating them
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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.
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