Development of New Prophylactic Radioprotective Agents
Final summary rept. 1 Dec 1983-31 Dec 1984
RESEARCH TRIANGLE INST (RTI) RESEARCH TRIANGLE PARK NC
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The study presented in this report is concerned with the preparation of analogs of S-2-3-aminopropylaminoethylphosphorothioic acid, H2NCH2CH2NHCH2CH2SPO3H2 WR2721, with modifications in the terminal amine function as potentially new prophylactic radioprotective agents. We have developed general methods for the synthesis of WR2721 analogs that possess amide -C-ONHR and thioamide -CSNHR terminal residues. The method has been used to prepare the following six target compounds CH3NHCO- CH2CH2NHCH2CH2SPO3HLi, C2H5NHCOCH2CH2NHCH2CH2SPO3HLi, CH3NHCSCH2CH2NHCH2CH2SPO3HLi, C2H5NHCSCH2CH2NHCH2CH2SPO3HLi, H2NCOCH2CH2NHCH2CH2SPO3Hi, and H2NCSCH2CH2NHCH2CH2SPO3HLi. Four of the above compounds were submitted to WRAIR for testing. The intermediate, BrCH2CH2NHCH2CH2CNHNHCH3.2HBr, required for hte synthesis of the WR2721 analog, CH3NHCNHCH2CH2NHCH2CH2SPO3H2 , was prepared and characterized.