Verfahren zur Herstellung von Uridin-Derivaten

The invention comprises 21-deoxy -5- fluoro-31, 51-di (O-acetyl)-uridine and the preparation thereof by acetylating 21-deoxy -5- fluoro-uracil, for example with at least 2 mols of an acylating agent such as acetic anhydride or acetyl chloride. The above process is useful for the preparation of pure 21-deoxy -5- fluoro-uridine-in particular free from 5-fluoro-uracil, by acetylating crude 21-deoxy -5- fluoro-uracil by the above method, isolating the di-O-acetyl compound free from the impurity, and hydrolysing the di-O-acetyl compound back to 21-deoxy -5- fluoro-uridine. 21-Deoxy -5- fluoro-uridine (containing some 5-fluoro-uracil) is prepared by growing cells of Escherichia coli, separating the cells by centrifuging, adding the cells to a mixture of 5-fluoro-uracil and thymidine in a buffered solution, incubating the resulting mixture, and separating the 5-fluoro-uracil from the filtered solution. Therapeutic compositions useful as an anti-metabolite and which may be administered orally contain as the active ingredient 21-deoxy -5- fluoro-31, 51-di (O-acetyl)-uridine.