| 摘要 |
NEW MATERIAL:2-Hydroxymethyl-3,3,3-trifluoropropionic acid shown by the formula I. USE:An intermediate capable of producing simply in high yield 5- trifluoromethyldihydrouracil suitable as an intermediate for trifluorothymidine (carcinostatic agent). PREPARATION:2-Trifluoromethylacrylic acid shown by the formula II is reacted with water in the presence of an acid such as hydrochloric acid, sulfuric acid, etc., especially sulfuric acid preferably at 90-130 deg.C to give a compound shown by the formula I. The compound is reacted with urea in dimethylformamide in the presence of acetic anhydride to give 5-perfluoromethyldihydrouracil shown by the formula III, which is reacted with bromine in acetic acid and heated to give trifluorothymine. This compound is condensed with a saccharide to synthesize trifluorothymidine.
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