| 摘要 |
<p>PURPOSE: To obtain the subject new derivative which is a specific anthracycline derivative containing 4-amino-2,4,6-trideoxy-2-fluoro-mannopyranosyl group, having a high water solubility and useful as an antitumor agent, etc., having excellent antitumor activities. CONSTITUTION: This new anthracycline derivative comprises a daunomycinone or an adriamycinone derivative (salt) of formula I (R is H or hydroxyl) having 4-amino-2,4,6-trideoxy-2-fluoro-mannopyranosyl group. The derivative has a high water solubility and excellent antitumor activities and is useful as an antitumor agent, etc. The compound derivative is obtained by carrying out the condensing reaction of daunomycinone of formula II with a compound of formula III (Y' is acetyl as a hydroxyl-protecting group; Y" is trifluoroacetyl or benzoyl as an amino-protecting group; X is Br or I) in the presence of a condensing catalyst in an organic solvent and then removing the protecting groups.</p> |
