Bleomycinic acid

In 400 ml of dimethylformamide was dissolved 15.0 g of bleomycinic acid (copper-containing form). To the solution kept at 0°C by cooling were added 1.1 ml of N-methylmorpholine and 10.3 g of 6-chloro-1 -p-chlorobenzenesulfonyloxybenzotriazole (CCBT) as an activating compound. The mixture was stirred for 5 minutes at 0°C, then admixed with 5.3 g of N-[(S)-1 -phenylethyl] -1 3-diaminopropane and further stirred for 1 hour. 

Using aqueous ammonium chloride solution, elution was performed by passing through the column 20 liters of eluent in which the concentration of ammonium chloride was continually increased from 0.05 to 1. OM. The unreacted bleomycinic acid was found in the effluent at the ammonium chloride concentration of about 0.05M and NK631 at the ammonium chloride concentration of about 0.45 M. Both fractions, which showed UV absorption at 292 m/u, were separately collected. 

By similar treatment, 280 mg of the unreacted bleomycinic acid (copper-containing form) were recovered. 

Bleomycinic acid Peplomycin sulfate Boric acid... 

The discovery of bleomycin in 1966 resulted from a program established by H. Umezawa to screen microbial culture filtrates against experimental tumors. Bleomycin is a mixture of closely related compounds that is partly resolved before formulation for clinical use. The presently used commercial product. Blenoxanc. contains bleomycins Aj and B2. A variety of other antibiotics have structures. similar to those of the bleomycins. They include the phleomycins (which differ from bleomycins in having one thiazolc ring partly reduced), zorbamycin and the zorbonamycins. antibiotic YA-S6, victomycin. the tallysomycins. and the pla-tomycin.s. New bleomycin analogues al.so have been pic-pared from bleomycinic acid by controlled bio.synthe.sis. 

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