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博莱霉素(Bleomycins)(Ⅰ)是一族性质近似的糖肽抗肿瘤抗菌素。本文报导,化学裂解(Ⅰ-a)成(Ⅰ-c)及新的半合成(Ⅰ)的制备。Ⅰ的分子中有许多可以水解的基团,作者选择性地水解Ⅰ-a末端肽键。选Ⅰ-a为原料因为它是(Ⅰ)的主要组分,而且在其胺基部分有一个活性锍基(Sulfonium)。直接从(Ⅰ-a)经环化亚氨基醚(Ⅱ)得极微量(Ⅰ-c)。
Bleomycins (Ⅰ) is a family of similar glycopeptide anti-tumor antibiotics. This paper reports the preparation of the chemical cleavage (I-a) into (I-c) and the new semisynthetic (I). There are many hydrolysable groups in the molecule of I, and the authors selectively hydrolyze the I-a terminal peptide bonds. I-a is the starting material because it is the major component of (I) and has an active sulfonium group in its amine moiety. A very small amount of (I-c) was obtained directly from (I-a) through the cyclized iminoether (II).