Synthesis and manufacture of pentostatin and its precursors, analogs and derivatives
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United States of America Patent
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Issued Date -
Dec 1, 2005
app pub date -
Sep 15, 2004
filing date -
Sep 15, 2003
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Abstract
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, especially pharmaceutically important heterocyclic compounds.
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