Synthesis of high specific activity (3,4-[3H]cyclohexyl)-N-[1 (2-benzo[b]thienyl)cyclohexyl]piperidine {[3H]BTCP}: A selective probe for the dopamine-reuptake complex |
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Authors: | Brian R. de Costa |
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Affiliation: | Laboratory of Medicinal Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892, U.S.A. |
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Abstract: | High specific activity [3H]BTCP, a radioligand for the dopaminereuptake complex was synthesized in 7-steps starting with the readily available starting materials, cyclohexane-1,4-dione monoethylene ketal and benzo[b]thiophene; the tritium label was introduced in the final step on the 3- and 4- positions of the cyclohexyl ring by catalytic tritiation of N-[4-(2-benzo[b]thienyl)cyclohexenyl]piperidine to give [3H]BTCP in 7.3% yield with a specific activity of 29.8 Ci/mmol (51.4% isotopic incorporation). |
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Keywords: | [3H]BTCP Radioligand Dopamine Reuptake Complex Cyclohexane-1,4-dione Monoethylene Ketal Benzo[b]thiophene N-[4-(2-Benzo[b]thienyl)cyclohexenyl]piperidine Catalytic Tritiation |
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