METHODS FOR PREPARING ANTHRACYCLINONE DERIVATIVES AND ANTHRACYCLINONE DERIVATIVES PER SE

摘要

The present invention relates to a process for preparation of a product compound of the Formula (I), where R1 is an acyl group, R2 is H, an N−alkylated amino sugar, or a non−basic sugar moiety, and R3 is H, OH, or OCH3. The process involves reacting a starting compound of the Formula (II) with an acyl donor compound in the presence of a non−chemically modified lipase, under conditions effective to produce the product compound. Another aspect of the present invention relates to a compound of the following Formula (III), where: R1 is an acyl radical of a carboxylic acid selected from the group consisting of: polyethylene glycol acetic acid and polyunsaturated fatty acid; and R2 = 2,6−dideoxy−2−fluoro−&agr;−talopyr anosyl; 3−trifluoroacetylamino−2,3,6−trideoxy&mi nus;&agr;−L−lyxo−hexopyranosyl; or 3−deamino−3−(2'−pyrroline−1&ap os;−yl)−2,3,6−trideoxy−&agr;& minus;L−lyxo−hexopyranosyl; or a pharmaceutically acceptable salt thereof. The present invention also relates to a compound of the Formula (IV) where n is 4 or 5, or a pharmaceutically acceptable salt thereof. Another aspect of the present invention relates to a compound of the Formula (V) where: R1 is an acyl group, R2 is 3−substituted allyloxycarbonylamino−2,3,6−trideoxy−&ag r;−L−lyxo−hexopyranosyl, R3 is H, OH, or OCH3.