An Efficient Method to Prepare 4-Aminoquinazolines: Potential Application to Conformation-Restricted Bleomycin Analogs

To enhance the iron-chelating ability of P-3A, 4-aminoquinazolines were designed as conformation-restricted bleomycin analogs. An efficient method was developed to prepare the 4-aminoquinazoline heterocyclic nucleus, which entails a two-step one-pot procedure leading to 4-aminoquinazolines in good yields. The application of this method to synthesis 4-aminoquinazoline bleomycin analogs is envisioned.