3 '-azido-2 ',3'-deoxyuridine (AZDU) has commercial potential as a therapeutic agent in the treatment of AIDS. At the present time it is produced via a complex expensive solution synthesis. The purpose of this Phase II SBIR research project is to investigate the scale-up potential of a solid phase synthesis procedure which has already been proven feasible in the laboratory under a Phase I grant. The motivation includes substantial savings in production costs and an environmentally benign process with minimal waste generation. The process for the solid state synthesis progresses in four stages: 1. Activation of the functionalized polymer support 2. Bonding of nucleoside to the resin 3. Conversion to polymer-bound AZDU 4. Product removal by hydrolysis with regeneration of the functionalized polymer Eventually production could be largely automated. There is a potential that in lots of several kilograms, AZDU can be produced by solid-phase technology for half of the cost required for the solution method.
