Preparation of Radiolabeled Compounds for the U.S. Army Drug Development Program.

This report summarized work carried out on contract DAMD17-93-C-3001 during the period November 15, 1995 to November 14, 1996. The purpose of the work on this contract is to prepare and fully characterize radiolabeled samples of compounds which are of current interest to the U.S. Army Medical Research and Materiel Command USAMRMC and to provide these compounds along with some commercially prepared compounds to investigators designated by the USAMRMC. The syntheses of carbon-14 labeled nitrogen mustard WR-1439, 14Chalofantrine WR-171669, 14Cdesbutylhalofantrine WR-178460, 14Cartemether WR-254986, and 14Cartelinic acid WR-255663 were completed during this report period. The synthesis of high specific activity tritium labeled artemisinin, and an alternate synthesis of carbon-14 labeled artemisinin were investigated. Resyntheses of 14Cmefloquin WR-142490 and 3Hpyridostigmine bromide WR-250710 were initiated. A total of nine shipments were made, three of which required purification prior to shipment.