503315-74-0Relevant articles and documents
Synthesis route and preparation method of 3-fluorine-4-nitrobenzaldehyde
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, (2021/01/28)
The invention discloses a new synthetic route of 3-fluorine-4-nitrobenzaldehyde and a preparation method thereof. The preparation method comprises the following steps: adding 3-fluorine-4-nitrobenzoicacid and an acidic catalyst into an organic solvent methanol, stirring at 60 to 80 DEG C for 5 to 12 hours, and carrying out after-treatment to obtain a solid intermediate product 2; adding the intermediate product 2 into an organic solvent II, adding sodium borohydride while uniformly stirring at 0 DEG C, stirring for 0.5 to 1h at 0 DEG C, slowly heating to 60 DEG C, stirring for 2 to 6h, stopping stirring, and carrying out post-treatment to obtain an intermediate product 3; and adding the intermediate product 3 and an oxidant III into an organic solvent IV, heating and refluxing for 3 to 10hours, cooling to 20 to 30 DEG C after the reaction is finished, and carrying out post-treatment on the reaction solution to obtain the product 3-fluorine-4-nitrobenzaldehyde. According to the methoddisclosed by the invention, sodium borohydride which is safe and easy to treat is adopted to replace high-activity ultralow-temperature anhydrous oxygen diisobutyl aluminum hydride for reduction reaction, so that a relatively good effect is achieved, and the compound 3-fluorine-4-nitrobenzaldehyde is safely and efficiently synthesized. The method is simple, the requirements of production equipment are reduced, the cost is controlled, and the method is suitable for industrial production.
Synthesis and Biological Characterization of Aryl Uracil Inhibitors of Hepatitis C Virus NS5B Polymerase: Discovery of ABT-072, a trans-Stilbene Analog with Good Oral Bioavailability
Randolph, John T.,Krueger, A. Chris,Donner, Pamela L.,Pratt, John K.,Liu, Dachun,Motter, Christopher E.,Rockway, Todd W.,Tufano, Michael D.,Wagner, Rolf,Lim, Hock B.,Beyer, Jill M.,Mondal, Rubina,Panchal, Neeta S.,Colletti, Lynn,Liu, Yaya,Koev, Gennadiy,Kati, Warren M.,Hernandez, Lisa E.,Beno, David W. A.,Longenecker, Kenton L.,Stewart, Kent D.,Dumas, Emily O.,Molla, Akhteruzzaman,Maring, Clarence J.
supporting information, p. 1153 - 1163 (2018/02/17)
ABT-072 is a non-nucleoside HCV NS5B polymerase inhibitor that was discovered as part of a program to identify new direct-acting antivirals (DAAs) for the treatment of HCV infection. This compound was identified during a medicinal chemistry effort to impr
Synthesis and structure-activity relationships of nitrobenzyl phosphoramide mustards as nitroreductase-activated prodrugs
Hu, Longqin,Wu, Xinghua,Han, Jiye,Chen, Lin,Vass, Simon O.,Browne, Patrick,Hall, Belinda S.,Bot, Christopher,Gobalakrishnapillai, Vithurshaa,Searle, Peter F.,Knox, Richard J.,Wilkinson, Shane R.
, p. 3986 - 3991 (2011/08/06)
A series of nitrobenzyl phosphoramide mustards and their analogs was designed and synthesized to explore their structure-activity relationships as substrates of nitroreductases from Escherichia coli and trypanosomes and as potential antiproliferative and antiparasitic agents. The position of the nitro group on the phenyl ring was important with the 4-nitrobenzyl phosphoramide mustard (1) offering the best combination of enzyme activity and antiproliferative effect against both mammalian and trypanosomatid cells. A preference was observed for halogen substitutions ortho to benzyl phosphoramide mustard but distinct differences were found in their SAR of substituted 4-nitrobenzyl phosphoramide mustards in E. coli nitroreductase-expressing cells and in trypanosomatids expressing endogenous nitroreductases.
