D-Galactopyranose as chiral inductor in the asymmetric synthesis of aziridine derivatives

摘要

Aziridine-containing natural products, such as azinomycins, mitomycins and related compounds exhibit antibiotic and antitumour activities of significant interest (1).Of these, azinomycins possess a broad spectrum of activity against cancers, and mitomycin C has been in clinical use since the 1960s for the treatment of a wide range of tumours. The activity of all these compounds lies in the role of aziridines as powerful alkylating agents. Furthermore, several synthetic aziridines have also been reported to exhibit useful biological properties such as irreversible inhibition of glutamate racemase, and diaminopimelic acid epimerase (DAP), and high level cytotoxicity against melanoma cell lines (2).