Synthetic method of sofosbuvir intermediate
2015
The invention relates to a synthetic method of sofosbuvir intermediate-(2'R)-N- benzoyl-2'-deoxy-2'-fluoro-2'-methylcytidine-3',5'-dibenzoate represented by a formula (I) (shown in the specification). The synthetic method comprises the steps of generating a reduction product compound IV of a compound III from the compound III in the presence of modified red aluminum, generating a chlorinated compound V from the compound IV through sulfoxide chloride chlorination under the catalysis of N,N-dimethylformamide, after separating organic materials and aluminum salt from the compound V, directly condensing the compound V with a compound VI N-benzoyl-O-(trimethylsilyl)cytosine, and carrying out hydrolysis by virtue of an acetic acid solution, so as to obtain (2'R)-N- benzoyl-2'-deoxy-2'-fluoro-2'-methylcytidine-3',5'-dibenzoate represented by the formula (I). The synthetic method has the advantages of high yield, convenience in operation and suitability in industrial production.
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