In our earlier communication, a Recently, we reported the ultra fast functionalization of controlled-pore glass (CPG) based on using microwave-assisted functionalization was reportedprocedures (Fig. 1). This method has providesd rapid access to aminated and subsequent succinylated CPG in multi-gram quantities (100g lots). Concurrently, we have also developed Recent studies from our laboratories focused on improving improved procedures for loading of nucleosides on to functionalized CPG. This led to the identification of N,N-dimethylformamide (DMF) as a more useful solvent than most commonly used pyridine and also to the design of a using a versatile multipurpose chemical synthesis reactor.
Fig. 1. Microwave-assisted functionalization of solid supports.
Using these modified conditions, functionalization and loading of nucleoside of other solid supports has also been carried out. Nucleoside-loaded CPG, obtained following these protocols, has been successfully used for the synthesis of the our lead anti-HBV molecule SB-9000. Results of our recent studies will be presented.
Acknowledgement: Support of this research from the National Institutes of Health, under a Research Project Cooperative Agreement Grant Award 5 UO1 AI058270-02, is gratefully acknowledged.
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Back to The 33rd Northeast Regional Meeting (July 14-17, 2005)