- Synthesis of [2H, 13C] and [14C] labeled vasopressin V1a/V2 receptor antagonist RWJ-676070 and its stable labeled N-des-benzoyl metabolite
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Stable isotope-labeled ([13C2, D3]) and carbon 14-labeled vasopressin receptor antagonist RWJ-676070, a spirobenzazepine amide, were prepared in separate syntheses for use in drug metabolism studies. The stable isotopically labeled sample was prepared starting from [ 13C2, D6]dimethyl sulfate and [ 13C]copper (I) cyanide in nine steps with a 14% overall isotopic yield. The 14C label was introduced in five steps starting from [14C]potassium cyanide to provide material having a specific activity of 58 mCi/mmol (2.15 GBq/mmol). Selective hydrolysis of the metabolically labile amide bond in [13C2, D3]RWJ-676070 gave the corresponding labeled metabolite in one step. Copyright
- Gong, Yong,Hoerr, David C.,Weaner, Larry E.,Lin, Ronghui
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p. 268 - 272
(2008/12/21)
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