100367-55-3Relevant articles and documents
The Synthesis of the High-Potency Sweetener, NC-00637. Part 2: Preparation of the Pyridine Moiety
Ager, David J.,Erickson, Robert A.,Froen, Diane E.,Prakash, Indra,Zhi, Ben
, p. 62 - 71 (2004)
The pyridine moiety within the high-potency sweetener, NC-00637 (1), 5-amino-2-cyanopyridine (4), was prepared from 2-hydroxy-5-nitropyridine (10). The sequence involved the conversion of the hydroxy group to bromide followed by substitution with cyanide to give 2-cyano-5-nitropyridine (8). Reduction of the nitro group proved to be troublesome when catalytic hydrogenation was used. Iron with an acid gave a reproducible reaction that could be used at scale.
Preparation method of 2-nitrile-5-hydroxypyridine
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Paragraph 0021; 0022; 0023, (2017/08/29)
The invention relates to a preparation method of 2-nitrile-5-hydroxypyridine. The method comprises the steps: taking 2-bromine-5-nitropyridine, NaCN, CuCN, dimethylformamide, KH2PO4 and the like as starting raw materials to generate 2-nitrile-5-nitropyridine, adding ethyl acetate, an appropriate amount of reduced Fe powder and an enough amount of acetic acid, adding an appropriate amount of H2SO4 solution and NaNO2, and performing filtering and drying to obtain orange-yellow solid 2-nitrile-5-hydroxypyridine. The method is mild in reaction condition and low in cost; the raw materials are easy to obtain; and the method is suitable for mass production of a plant.
NOVEL AZA-OXO-INDOLES FOR THE TREATMENT AND PROPHYLAXIS OF RESPIRATORY SYNCYTIAL VIRUS INFECTION
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Page/Page column 27; 28, (2015/02/25)
The invention provides novel compounds having the general formula: wherein R1, R2, R3, R4, R5, W and X are as described herein, compositions including the compounds and methods of using the compounds.
Discovery of inhibitors of aberrant gene transcription from libraries ofdna binding molecules: Inhibition of LEF-1-mediated gene transcription and oncogenic transformation
Stover, James S.,Shi, Jin,Jin, Wei,Vogt, Peter K.,Boger, Dale L.
supporting information; experimental part, p. 3342 - 3348 (2009/07/30)
The screening of a >9000 compound library of synthetic DNA binding molecules for selective binding to the consensus sequence of the transcription factor LEF-1 followed by assessment of the candidate compounds in a series of assays that characterized functional activity (disruption of DNA-LEF-1 binding) at the intended target and site (inhibition of intracellular LEF-1-mediated gene transcription) resulting in a desired phenotypic cellular change (inhibit LEF-1-driven cell transformation) provided two lead compounds: lefmycin-1 and lefmycin-2. The sequence of screens defining the approach assures that activity in the final functional assay may be directly related to the inhibition of gene transcription and DNA binding properties of the identified molecules. Central to the implementation of this generalized approach to the discovery of DNA binding small molecule inhibitors of gene transcription was (1) the use of a technically nondemanding fluorescent intercalator displacement (FID) assay for initial assessment of the DNA binding affinity and selectivity of a library of compounds for any sequence of interest, and (2) the technology usedto prepare a sufficiently large library of DNA binding compounds.
