PURPOSE: To provide novel compounds possessing excellent antifungal activity and moreover, improved water solubility and useful for treatment of fungal infection.
CONSTITUTION: By reacting pradimicin A of formula II (wherein X represents H and Y represents methyl) with a silylating agent, preferably N,O-bis(trimethylsilyl)acetoamide, in an organic solvent such as THF at a temperature of from 5°C to 50°C for from 5 minutes to 1 hour, thereafter, reacting the reaction mixture with cyanobromide at a room temperature, finally treating the reaction product with hydrochloric acid in methanol and thereafter, treating it through column chromatograpy, the compounds of formula I (wherein R1 represents H, methyl or hydroxymethyl, provided that the produced amino acid residue takes D-configuration when R1 is other than H; R2 represents H or β-D-xylosyl; R3 represents H or alkyl; R4 represents -CN, -NO, -CH=NH or the like) or salts thereof is obtained.
HIRANO MINORU
MASUKICHI SHINJI
