379270-35-6Relevant academic research and scientific papers
Preparation method of tenofovir alafenamide intermediate
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, (2021/02/24)
The invention belongs to the technical field of medicinal chemistry, and provides a preparation method of a tenofovir alafenamide intermediate. The method comprises the following steps: reacting tenofovir serving as a raw material with an alkali or an salt of an alkali metal to a generate tenofovir alkali metal single salt, and reacting the tenofovir alkali metal single salt with triphenyl phosphite to generate a target intermediate. According to the invention, the method has the advantages of simple reaction conditions, high raw material utilization degree, high yield, high purity, reductionof the use of a large amount of organic bases, less generated waste liquid, small environmental pollution, and suitableness for industrial production.
Preparation method of tenofovir prodrug intermediate GS101
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Paragraph 0007-0035, (2021/09/26)
The invention relates to a preparation method of a tenofovir prodrug intermediate GS101, and belongs to the field of organic synthesis. The method comprises the following steps. The preparation method is mild in reaction condition, and the obtained product is good in purity and high in yield.
Industrial synthesis method of propofovir disoproxil fumarate
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Paragraph 0043-0046, (2021/01/29)
The invention provides a preparation process of propofovir disoproxil fumarate, which is short in production period, simple to operate and suitable for industrial production, and the high-purity propofovir disoproxil fumarate is prepared by taking the propofovir disoproxil fumarate as a starting material through special phosphorus chiral atom synthesis, purification and separation. The purity of the prepared propofovir disoproxil fumarate is greater than 99.90%, the diastereoisomer is less than 0.15%, the content of other single impurities is less than 0.10%, and the method has high commercialscale production value.
Preparation method of intermediate GS102 of tenofovir prodrug
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Paragraph 0008, (2021/02/13)
The invention relates to a preparation method of an intermediate GS102 of a tenofovir prodrug. A product obtained by the method is good in purity and high in yield.
Preparation method of intermediate GS103 of tenofovir prodrug
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Paragraph 0007, (2021/02/13)
The invention relates to a preparation method of an intermediate GS103 of a tenofovir prodrug. A product obtained by the method is good in purity and high in yield.
Preparation method of tenofovir alafenamide
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Paragraph 0021-0023, (2020/11/26)
The invention discloses a preparation method of tenofovir alafenamide. According to the method, n-butyl acetate is used as a solvent in the synthesis process of an intermediate, namely [[(1R)-2-(6-amino-9H-purin-9-yl)-1-methylethyoxyl]methyl]monophenyl ph
Tenofovir alafenamide diastereoisomer, preparation method and application of diastereoisomer
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Paragraph 0049-0051, (2020/09/16)
The invention relates to a tenofovir alafenamide diastereomer as shown in a formula I. The invention also relates to a preparation method of the tenofovir alafenamide diastereoisomer as shown in the formula I, and application of the tenofovir alafenamide diastereomer in detection of purity of the tenofovir alafenamide and salt thereof, detection of content of optical isomers in the tenofovir alafenamide and salt thereof, and quality control in production or preparation of the tenofovir alafenamide and salt thereof. The tenofovir alafenamide diastereomer disclosed by the invention has importantsignificance for quality monitoring and standard research in industrial production of tenofovir alafenamide.
Method for synthesizing tenofovir monophenyl ester
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Paragraph 0029-0031, (2020/08/18)
The invention discloses a method for synthesizing tenofovir monophenyl ester. The method comprises the following steps: adding tenofovir (PMPA), diphenyl iodonium salt, an acid-binding agent and a solvent into a reaction bottle, reacting for a period of time, performing detection, if the solvent is a non-water-soluble solvent, adding diluted hydrochloric acid to adjust the pH value to be below 1 after reaction, layering, adding sodium carbonate into a water layer for neutralization to adjust the pH to 2-3, separating out a solid, and performing filtering. If the solvent is a water-soluble solvent, dichloromethane and diluted hydrochloric acid need to be added to adjust the PH to be below 1, an organic layer is extracted and separated out, sodium carbonate is added to a water layer for neutralization to adjust the pH to 2-3, solid is separated out, filtered and dried, and tenofovir monophenyl ester is obtained. The method has the advantages of being high in yield, easy to operate, few in three wastes and the like.
Nucleotide phosphonate monohydrate as well as preparation method and application thereof in medicine
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Paragraph 0034; 0038; 0049-0054, (2020/03/17)
The invention relates to a monohydrate of a compound (I) and a preparation method thereof, and a composition and application thereof in preparation of drugs for treatment of viral infectious diseases.
Preparation methods of tenofovir alafenamide fumarate isomer impurities
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Paragraph 0083; 0084, (2020/07/13)
The invention discloses preparation methods of tenofovir alafenamide fumarate isomer impurities, which comprise preparation methods of four isomer impurities, specifically, preparation methods of 9-{(R)-2-[((R)-{[(R)-1-(isopropoxycarbonyl) ethyl] amino}-phenoxy phosphoryl) methoxy] propyl} adenine, 9-{(R)-2-[((R)-{[(S)-1-(isopropoxycarbonyl) ethyl] amino}-phenoxy phosphoryl) methoxy] propyl} adenine, 9-{(R)-2-[((S)-{[(R)-1-(isopropoxycarbonyl) ethyl] amino}-phenoxy phosphoryl) methoxy] propyl} adenine and 9-{(S)-2-[((R)-{[(R)-1-(isopropoxycarbonyl) ethyl] amino}-phenoxy phosphoryl) methoxy] propyl} adenine. The preparation methods of tenofovir alafenamide fumarate isomer impurities have the beneficial effects that the methods are simple and easy to implement, raw materials are easy to obtain, conditions are mild, cost is low, production is facilitated, and meanwhile the obtained isomer impurity has important significance in preparing high-purity tenofovir alafenamide fumarate.
