Synthetic studies on an antitumor antibiotic, bleomycin. XIV. The synthesis of Boc-pyrimidoblamic acid.

Abstract

New methodology was developed for the introduction of an acetate unit into the Schiff base 2, based on the reaction of the Schiff base 2 with malonic acid monoester or vinyloxyborane. Furthermore, the synthesis of Boc-pyrimidoblamic acid, a key fragment for the total synthesis of bleomycin, was achieved by utilizing these two methods.