- Synthesis route and preparation method of 3-fluorine-4-nitrobenzaldehyde
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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.
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Paragraph 0004; 0011; 0013; 0016; 0018-0019
(2021/01/28)
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- Novel compounds that are inhibitors of YAP/TAZ-TEAD interaction and their use in the treatment of malignant mesothelioma
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These compounds are useful as inhibitors of the YAP/TAZ-TEAD interaction.
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Paragraph 0521-0523
(2020/02/01)
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- 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
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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
- 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.
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supporting information
p. 1153 - 1163
(2018/02/17)
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- Synthesis and structure-activity relationships of nitrobenzyl phosphoramide mustards as nitroreductase-activated prodrugs
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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.
- 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.
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scheme or table
p. 3986 - 3991
(2011/08/06)
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- COMPOUNDS, COMPOSITIONS AND METHODS FOR TREATMENT OF PROTOZOAN INFECTIONS
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Provided are compounds, compositions and methods for treating protozoan infections.
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Page/Page column 16
(2011/06/23)
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- N-PHENYL-DIOXO-HYDROPYRIMIDINES USEFUL AS HEPATITIS C VIRUS (HCV) INHIBITORS
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This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such interm
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Page/Page column 140
(2009/04/25)
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- AZOLIDINONE-VINYL FUSED-BENZENE DERIVATIVES
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The present invention is related to azolidinedione-vinyl fused-benzene derivatives of formula (I) for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, graft rejection or lung injuries. Formula (I), wherein A, X, Y, Z, R1 , R2 and n are as described in the description.
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