PREPARATION OF SYNTHETIC NUCLEOSIDES VIA p-ALLYL TRANSITION METAL COMPLEX FORMATION

This invention provides highly regioselective and stereoselective processes for preparing synthetic nucleosides. A process for the preparation of synthetic nucleosides is provided that comprises a) preparing a bicycloamide derivative, b) reacting the bicycloamide derivative with a nucleic acid base or heterocyclic base or salt thereof in the presence of a transition metal catalyst to form a cyclopentenecarboxamide, and c) cleaving a carboxamide group from the cyclopentenecarboxamide to form the synthetic nucleoside. The processes according to the invention can be used for the synthesis of a variety of anti-viral agents, including Abacavir, Carbovir, and Entecavir, as well as derivatives thereof.

Patents:
WO 2,009,021,114

Inventor(s): LIOTTA DENNIS C [US]; LI YONGFENG [US]

Type of Offer: Licensing



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