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filingDate 2018-03-26-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2020-06-09-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2020-06-09-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber CN-108440613-B
titleOfInvention Synthesis process of (2'R) -2' -deoxy-2 '-fluoro-2' -methyluridine
abstract The invention discloses a synthesis process of (2'R) -2' -deoxy-2 '-fluoro-2' -methyluridine, relates to the technical field of medicine synthesis, and solves the technical problems of high cost and low product yield of the existing process. According to the invention, sodium borohydride or potassium borohydride is used for reducing the ribose lactone, so that the use of expensive reducing reagent of red aluminum or lithium tri-tert-butoxy aluminum hydride is avoided, and the cost is greatly reduced; the N, O-bis (trimethylsilyl) acetamide is used as a silicon etherification reagent to improve the yield of the glycosylation reaction, the product yield can reach 85-90 percent and is far higher than 58 percent of the product yield in the third route, and the product yield is obviously improved; side reactions in the ring closure reaction can be avoided by protecting the hydroxyl at the 5' -position, and meanwhile, the product yield can reach 87-92% under the catalysis of sodium bicarbonate by using a common polar solvent, namely dimethylformamide. The synthesis process is easy to operate, the process conditions are easier to control, the cost is reduced, and the method is suitable for mass production.
priorityDate 2018-03-26-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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