Synthesis of N-desmethyl derivatives of 17alpha-acetoxy-11beta-(4-N,N-dimethylaminophenyl)-19-norpregna-4,9-die ne-3,20-dione and mifepristone1: substrates for the synthesis of radioligands. |
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| Authors: | P N Rao C K Acosta J W Cessac M L Bahr H K Kim |
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| Institution: | Department of Organic Chemistry, Southwest Foundation for Biomedical Research, San Antonio, TX 78245-0549, USA. |
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| Abstract: | The syntheses of N-desmethyl derivatives of CDB-2914 and the mono-N-desmethyl derivative of Mifepristone are described. We also describe the use of the mono-desmethyl derivatives as substrates for the synthesis of N-tritomethyl derivatives of CDB-2914 and Mifepristone with high specific activity (ca. 80 Ci/mmol), which serve as radioligands for radioimmunoassay. |
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