| 摘要 |
NEW MATERIAL:A hitachimycin derivative shown by formula I (R1 and R2 are H or 2-6C alkanoyl with the proviso that R1 and R2 are neither H nor acetyl at the same time). EXAMPLE:11,15-Di-O-propionylhitachimycin. USE:An antibiotic having excellent antitumor activity. PREPARATION:Hitachimycin is reacted with an acyl halide of a carboxylic acid shown by the formula CnH2n+1CO2H (n is 1-5 integer) or an acid anhydride in the organic solvent containing no active hydrogen atom in the presence of a base at 10-90 deg.C for 6-48 hours to give a compound shown by formula II (R1=R2=2-6C alkanoyl), which is reacted in an organic solvent in the presence of an acid or a base at 0-60 deg.C for 1-30min to give a compound shown by formula III. Further this compound is acylated by the use of an acylating agent different from the above-mentioned acylating agent in the same way as above-mentioned to give a compound shown by formula IV (R1 and R2 are 2-6C alkanoyl and R1not equal to R2).
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