Synthesis and manufacture of pentostatin and its precursors, analogs and derivatives

Abstract From the Canadian patent

Methods and compositions are provided for efficiently preparing and manufacturing pentostatin. Also provided are novel precursors of pentostatin pentostatin analogs and derivatives. In one aspect of the invention a method , is provided for total chemical synthesis of pentostatin via a route of heterocyclic ring expansion. For example a heterocyclic pharmaceutical , intermediate for drugs such as pentostatin e.g. the diazepinone precursor, can be obtained efficiently through a ring expansion of an O-C-N functionality in a hypoxanthine or 2'-deoxyinosine derivative. The methods and compositions can also be used to synthesize and manufacture heterocyclic compounds other than pentostatin, …