911208-73-6Relevant academic research and scientific papers
Novel antiviral nucleoside reverse transcriptase inhibitor
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Paragraph 0311; 0314; 0319; 0320, (2019/04/06)
The invention relates to a novel antiviral nucleoside reverse transcriptase inhibitor compound, a pharmaceutical composition comprising the same and preparation and application thereof. Particularly,the invention discloses a condensed pyrimidine compound
Improved method for synthesis technology of n-hexadecyloxypropyl tenofovir disoproxil
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Paragraph 0011; 0035; 0036, (2018/06/15)
The invention discloses an improved method for a synthesis technology of n-hexadecyloxypropyl tenofovir disoproxil, and belongs to the technical field of organic synthesis. The method comprises the following steps: 1, reacting n-hexadecyl bromide (2) with 1,3-propylene glycol (3) to obtain 3-n-hexadecyloxypropanol (4); 2, chlorinating PMPA (5) to obtain an acyl chloride intermediate (6); 3, esterifying the acyl chloride intermediate (6) and the 3-n-hexadecyloxypropanol (4) to obtain an intermediate (7); and 4, hydrolyzing and re-crystallizing the intermediate (7) to obtain the n-hexadecyloxypropyl tenofovir disoproxil (1), wherein the total yield is about 62%, and the purity is more than 99%. The method mainly has the advantages of easily available materials, simplicity in operation, low cost, and facilitation of industrial production.
Nucleoside phosphoramidate type compound with HBV/HIV resistance activity and salt and application of nucleoside phosphoramidate type compound
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Paragraph 0070, (2017/08/28)
The invention relates to a nucleoside phosphoramidate type compound with HBV/HIV resistance activity, an isomer of the nucleoside phosphoramidate type compound, pharmaceutically-acceptable salt of the nucleoside phosphoramidate type compound, a solvate or crystal of the nucleoside phosphoramidate type compound, a medicine composition of the nucleoside phosphoramidate type compound, and application of the nucleoside phosphoramidate type compound. According to related novel non-cyclic nucleoside phosphoramidate, on the phosphoramidate part, amino acid is D-amino-acid. D-amino-acid ester is introduced in the prodrug, and a new non-cyclic nucleotide amide compound which has higher chemical stability, higher lipid solubility and higher virus inhibition activity is expected to be obtained. By means of the creative design, the virus resistance activity of medicine is improved, solubility and pharmacokinetics characteristics of the medicine are improved, the concentration ratio in tissue cells and plasma is increased, and therefore the curative effect, safety and tolerance of the medicine can be improved, and very good clinical application prospects are achieved.
