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filingDate 2012-02-22-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_34426cdf4e023d50c627c3aadebafc49
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publicationDate 2013-09-11-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber CN-103288905-A
titleOfInvention Novel technology for synthesis of capecitabine
abstract The invention relates to a novel technology for synthesis of capecitabine. The technology is characterized in that: 5-fluorocytosine protected by trimethyl silicon is taken as raw material; and the capecitabine is obtained after condensation, esterification and deacetylation. The Reaction sequence is more economically reasonable, the synthetic route is short, the cost is low, the operation is simplified, the yield is high, the synthetic period is short, the quality of intermediates can be controlled, solvents used in reaction are few, pollution to the environment is little, and the technology is suitable for industrial production. Comparing the technology with the prior art for capecitabine production, trimethylsilyl trifluoromethanesulfonate (TMSOTf) which replaces a heavy metal agent stannic chloride is used as a condensing agent for glycosylation (condensation), and a sodium methoxide/methanol system replaces an ammonia gas/methanol system for deacetylation, so that the production yield is increased, and heavy metal residues of the products and the environmental pollution are reduced. The overall yield of the technology of the invention reaches 59%, the purity of the production is high and meets the standards of the United States Pharmacopeia.
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priorityDate 2012-02-22-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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