Solid-Phase Synthesis of Bleomycin Group Antibiotics. Elaboration of Deglycobleomycin A5

Abstract
The solid-phase syntheses of two deglycobleomycin A5 analogues were achieved using a commercially available polystyrene resin containing triphenylmethyl-linked spermidine. The final products were deblocked and released from the resin, analyzed, and purified by C18 reversed phase HPLC and characterized by high-field 1H NMR spectroscopy and mass spectrometry. The purified products relaxed supercoiled plasmid DNA in a concentration-dependent fashion and to the same extent as authentic material derived from natural BLM A5.