RESUMEN
The synthesis of [N-methyl-3 H](+/-)-mecamylamine is described as an example of a convenient and mild method to reduce formamide groups using tritiated borane generated in situ. The product was characterized by thin layer chromatography, high performance liquid chromatography, mass spectrometry, and tritium NMR.
RESUMEN
Loperamide is a piperidine butyramide mu-opiate receptor agonist and currently employed to treat diarrhea. Because a single past report of tritiating loperamide was limited to only a very low specific activity product without technical details or extensive analysis, the synthesis of [N-methyl-(3)H]loperamide at high specific activity is now described in detail. An imine precursor was alkylated with [(3)H]methyl iodide to obtain a quaternary intermediate, which was then reacted with 4-(4-chlorophenyl)-4-hydroxypiperidine to afford the desired product [N-methyl-(3)H]loperamide, characterized by thin layer chromatography (TLC), HPLC, MS, UV, and proton-decoupled tritium NMR.
Asunto(s)
Loperamida/química , Loperamida/síntesis química , Radioquímica , Técnicas de Química Sintética , Piperidinas/química , TritioRESUMEN
Methods are presented to synthesize and characterize [(3)H] tryptamine (1b) and [(3)H] etodolac (2c).
Asunto(s)
Etodolaco/química , Marcaje Isotópico/métodos , Tritio , Triptaminas/químicaRESUMEN
Methods are presented to synthesize and characterize [(3)H] mirfentanil and [(3)H] A-4334.
Asunto(s)
Fentanilo/análogos & derivados , Marcaje Isotópico/métodos , Pirazoles/química , Tiazoles/química , Tritio , Fentanilo/químicaRESUMEN
Methods are presented to tritiate and characterize colforsin analogues 2 and 3.
Asunto(s)
Colforsina/análogos & derivados , Colforsina/química , Colforsina/aislamiento & purificación , Marcaje Isotópico/métodos , Radiofármacos/química , Radiofármacos/aislamiento & purificación , Tritio/química , Tritio/aislamiento & purificación , Conformación MolecularRESUMEN
Valuable antiviral compound WIN 54954 was tritiated at high specific activity and the product was characterized.
Asunto(s)
Antivirales/síntesis química , Isoxazoles/síntesis química , Tritio , Indicadores y Reactivos , Isoxazoles/uso terapéutico , Técnica de Dilución de RadioisótoposRESUMEN
Tacrine and its analogues have shown promise as cognition enhancers and potential chemotherapeutic agents for Alzheimer's disease. [3H]tacrine was required to explore its mechanism of action via receptor binding assay and the radioligand was prepared by means of catalytic dehalogenation of several brominated precursors.
