- Preparation method of 2-aminobenzoxazole compound
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The present invention relates to a method for preparing a 2-aminobenzoxazole compound. Comprising the following steps: (1) condensation reaction: taking o-aminophenol and nitrobenzoyl chloride compounds as raw materials, synthesizing amide intermediates in an alkaline solution system. The highly selective double-base combination system does not react with the raw material and can neutralize the acid gas generated by the reaction; (2) Cyclization reaction: acid is added to the condensation reaction solution as a catalyst, and 2-nitrobenzoxazole compounds are generated after dehydration. The solid super acid catalyst used is efficient and easy to separate and recycle; (3) hydrogenation hydrogenation reaction: 2-nitrobenzoxazole compounds are catalyzed to obtain 2-aminobenzoxazole compounds. The bi-alkali system and solid super acids used in the present invention are highly selective, product quality and yield are high. The operation is safe and simple, the raw material cost is low, in line with the green and environmentally friendly production concept, which is conducive to industrial production.
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- Benzoxazole ionic compound, PBO fiber emulsion sizing agent containing benzoxazole ionic compound and preparation method of PBO fiber emulsion sizing agent
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The invention discloses a benzoxazole ionic compound shown as a formula X, a sizing agent containing the compound, and a preparation method and application of the sizing agent. The benzoxazole ionic compound shown in the formula X is similar to the PBO fiber in chemical structure, the compatibility of the sizing agent and the PBO fiber can be improved, and the preparation process is simple and easy to operate. According to the sizing agent, the problems that an existing sizing agent is poor in compatibility with the PBO fiber, a large number of flammable and combustible organic solvents need to be used in the sizing agent, and nano reinforcements in the sizing agent are difficult to effectively cover the surfaces of the fibers are solved. The sizing agent takes water as a solvent, is greenand efficient, is simple and environment-friendly to prepare, and not only can keep the original tensile strength of PBO fibers, but also can remarkably improve the IFSS of the composite material.
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Paragraph 0118-0119
(2020/11/05)
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- Preparation method of 2-(aminophenyl)-5-aminobenzoxazole
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The invention discloses a preparation method of 2-(aminophenyl)-5-aminobenzoxazole. The preparation method concretely comprises the following steps: (1) condensing sodium 2-amino-4-nitrophenolate andnitrobenzoyl chloride to obtain an ester intermediate; (2) cyclizing the ester intermediate under the catalysis of a strong acid to obtain 2-(nitrophenyl)-5-nitrobenzoxazole; and (3) hydrogenating the2-(nitrophenyl)-5-nitrobenzoxazole under the catalysis of Pd/C to obtain the 2-(aminophenyl)-5-aminobenzoxazole. The sodium 2-amino-4-nitrophenolate and nitrobenzoyl chloride are condensed to only generate a hydroxyl-substituted acylation intermediate (that is the ester intermediate), and the amino part does not react with the nitrobenzoyl chloride, so no amide impurities are generated, the reaction selectivity is high, the yield of condensation and cyclization is up to about 90%, and the purity of the above nitro compound is about 99%.
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- INHIBITORS OF HEPATITIS C VIRUS REPLICATION
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The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
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Paragraph 0597-0598
(2019/05/15)
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- Preparation method of diamido nitrogen-containing aromatic heterocycle compound
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The invention relates to the technical field of synthesis of compounds, in particular to a preparation method of diamido nitrogen-containing aromatic heterocycle compound. The preparation method includes mixing a compound having the structure as shown as the formula (I) with inorganic acid, reacting to obtain water-soluble organism, performing reduction reaction with a reducing agent sulfide to effectively reduce nitro-organism into amino-compounds, performing neutral reaction with alkali liquor so as to obtain the diamido nitrogen-containing aromatic heterocycle compound having the structureas shown as the formula (II) and having high yield and purity. The preparation method is simple and environmental friendly, is low in cost, needs mild reaction conditions, and is suitable to be popularized and applied in scale. According to tests, the yield of the diamido nitrogen-containing aromatic heterocycle compound prepared by the method is not lower than 90%, and even can reach 96%, and itspurity can reach 99.9%.
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Paragraph 0082; 0083; 0084
(2018/10/19)
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- METHOD FOR MANUFACTURING BENZOXAZOLE COMPOUNDS
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A method for manufacturing benzoxazole compounds is provided and has steps of: processing a reaction between o-aminophenol or a derivative thereof and an acyl chloride compound, so as to obtain a first product; and adding the first product into a solution of polyphosphoric acid to carry out a cyclization, so as to form a benzoxazole compound.
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- Synthesis and Preliminary Biologic Evaluation of 5-Substituted-2-(4-substituted phenyl)-1,3-Benzoxazoles as A Novel Class of Influenza Virus A Inhibitors
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The diversity-oriented chemistry synthesis together with the random screening approach has permitted the discovery and optimization of novel antiviral lead compounds. In this paper, a series of novel 5-substituted-2-(4-substituted phenyl)-1,3-benzoxazoles was synthesized and evaluated for their in vitro anti-influenza A virus and anti-influenza B virus activity. The activity was monitored by the MTS assay in the Madin-Darby canine kidney cells. Compound 7h showed excellent inhibitory activity and selective index against A/H3N2 (EC50=37.03μm, SI>5), which were all higher than that of the reference drug oseltamivir (EC50>59.00μm, SI>1). However, no compound displays inhibitory activity against influenza B virus.
- Li, Zhenyu,Zhan, Peng,Naesens, Lieve,Vanderlinden, Evelien,Liu, Ailin,Du, Guanhua,De Clercq, Erik,Liu, Xinyong
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experimental part
p. 1018 - 1024
(2012/07/30)
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- INHIBITORS OF HEPATITIS C VIRUS REPLICATION
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The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
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Page/Page column 83
(2010/11/04)
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- Process for making 2-aryl benz (ox, thi, imid) azoles and 2-aminoaryl aminobenz (ox, thi, imid) azoles
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2-(aryl)-benz(ox, thi, imid)azoles are prepared by reacting an aromatic aldehyde with hydroxylamine to form an aromatic aldehyde oxime, halogenating the oxime to form an aromatic hydroxamoyl halide, and then reacting this halide with certain aromatic amine compounds. The products may be nitrated and then reduced to form the corresponding diamines, which are useful in making PIBX polymers.
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- Preparation of an aminoarylaminoarazole
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An aminoarylaminoarazole can be prepared by a process comprising the steps of condensing a condensable nitroarylcarbonyl compound with an aminonitroarylol, an aminonitroarylthiol, or a triaminonitroarene to form a dinitroanilide, then reducing and cyclizi
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- Process for making 2-aryl benz (ox, thi, imid)azoles and 2-aminoaryl aminobenz(ox, thi, imid)azoles
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2-(aryl)-benz(ox, thi, imid)azoles are prepared by reacting an aromatic aldehyde with hydroxylamine to form an aromatic aldehyde oxime, halogenating the oxime to form an aromatic hydroxamoyl halide, and then reacting this halide with certain aromatic amine compounds. The products may be nitrated and then reduced to form the corresponding diamines, which are useful in making PIBX polymers.
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