AZDU, the dimethyl analog of AZT, is slated for clinical testing as a therapeutic in the treatment of AIDS. The current production of AZT is by the solution method and what small amounts have been made of AZDU have also been made via the solution method. Isolation and purification of the product is expensive, labor-intensive and results in substantial losses. Maximum yield that can be realized is around 40%. The objective of this research is to develop an alternative, more efficient process for the production of AZDU. It is based on the basic principle that product isolation from a reaction mixture is trivial if the product is attached to an insoluble polymer. Isolation then involves nothing more than a simple filtration of the resin. During Phase I of this Small Business Innovation Research project the possibility of making AZDU on a resin support will be explored. Specifically the PI will attempt to (1) select a suitably functionalized polymer to act as insoluble support in the conversion of deoxyuridine to AZDU, (2) effect the synthesis of AZDU on several samples of polymer in at least respectable yield, (3) learn enough about the kinetics of the individual steps to plan optimization for the future work of Phase II, and (4) generate a base set of quantitative data for a preliminary economic analysis, i.e. materials use, yield, polymer recycle, etc.
