Preparation of Radiochemical-Labeled Compounds for the U.S. Army Drug Development Program
Annual rept. 23 Mar 1991-22 Mar 1992
RESEARCH TRIANGLE INST (RTI) INST RESEARCH TRIANGLE PARK NC
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This report summarizes work carried out on contract DAMD17-89-C-9062 during the period March 23, 1991 to March 22, 1992. The purpose of the work on this contract was to prepare and fully characterize radiolabeled samples of compounds which are of current interest to the U.S. Amy Medical Research and Development Command USARMDC and to provide these compounds along with some commercially prepared compounds to investigators designated by the USARMDC. The procedure followed for preparing the compounds involved first designing a synthetic scheme and then optimizing the individual reactions in the synthetic scheme using nonlabeled chemicals. When all of the reactions had been optimized, a tracer run was done where a small amount of the radiolabeled starting material was diluted with nonlabeled starting material, and the reaction sequence performed from beginning to end on the exact scale that was planned for the master run. Any problems which were discovered in the tracer run were worked out, and then the tracer run was repeated, if necessary, or the master run was done. The final products were analyzed for chemical and radiochemical purity, and specific activity. Procedures used for the analyses included TLC-radio-scan, autoradiography, HPLC, UV, and NMR and mass spectrometry where required. In addition to analyzing the compounds when they were first prepared, they were also analyzed prior to shipment to approved investigators. Antimalarial, carbon- 14, tritium, synthesis, radiolabel, chemical warfare protective agents RAD 5, 1.
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