863329-66-2Relevant articles and documents
Preparation method of intermediate
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Paragraph 0030-0035; 0040-0043, (2021/09/08)
The invention relates to the field of pharmacy, in particular to a preparation method of an intermediate of a solovir intermediate (2 ’ R) -2 ’ - deoxidized -2 ’ -fluoro -2 ’ -methyl urea, and a compound represented by the formula II is reacted with triethylamine/methanol to generate a dehydroxylation protection reaction. By adopting the technical scheme disclosed by the invention, the total yield is high, the purity of the target product is high, the product stability is good, and the method is suitable for large-scale production. , Due to the fact that the adopted raw material cost is low, the process conditions are mild and non-rigorous, the method is easy to operate and easy to popularize.
Preparation method of anti-hepatitis C medicine sofosbuvir
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Paragraph 0052; 0071-0072, (2020/07/02)
The invention discloses a preparation method of an anti-hepatitis C medicine sofosbuvir. The method comprises the following steps: taking r-ethyl glycerate acetonide as an initial raw material, enabling the r-ethyl glycerate acetonide to react with ethyl alpha-fluoropropionate under the action of potassium tert-butoxide, performing carbonyl reduction, hydroxyl acylation, hydrolytic cyclization under an acidic condition, hydroxyl acylation, red aluminum reduction and chiral column separation so as to obtain a sofosbuvir key intermediate ((2R,3R,4R,5R)-3-(benzoyloxy)-5-hydroxy-4-fluoro-4-methyltetrahydrofuran-2-yl) methyl benzoate, performing 2-hydroxyl acetylation, enabling acetylized material to react with 2-trimethylsiloxy-4-benzamidopyrimidine, removing benzamido under an acidic condition, performing dehydroxylation protection, and finally enabling obtained material to react with N-[(S)-(2,3,4,5,6-Pentafluorophenoxy)phenoxyphosphinyl]-L-alanine 1-methylethyl ester to obtain the sofosbuvir. The method has the advantages of short synthesis route, high yield, avoidance of a fluorination reaction step in the synthesis process, and mild synthesis reaction conditions.
AN IMPROVED PROCESS FOR THE PREPARATION OF SOFOSBUVIR
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, (2018/02/20)
The present invention relates to an improved, commercially viable and industrially advantageous process for the preparation of Sofosbuvir. The present invention involves use of reagents that are less expensive, easier to handle and eco-friendly process.