SYNTHESIS OF HIGH SPECIFIC ACTIVITY (3,4-[H-3]CYCLOHEXYL)-N-[1(2-BENZO[B]THIENYL)CYCLOHEXYL]PIPERIDINE ([H-3]BTCP) - A SELECTIVE PROBE FOR THE DOPAMINE-REUPTAKE COMPLEX

被引:6
作者
DECOSTA, BR
机构
[1] Laboratory of Medicinal Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland
关键词
H-3]BTCP; RADIOLIGAND; DOPAMINE REUPTAKE COMPLEX; CYCLOHEXANE-1,4-DIONE MONOETHYLENE KETAL; BENZO[B]THIOPHENE; N-[4-(2-BENZO[B]THIENYL)CYCLOHEXENYL]PIPERIDINE; CATALYTIC TRITIATION;
D O I
10.1002/jlcr.2580290207
中图分类号
Q5 [生物化学];
学科分类号
071010 ; 081704 ;
摘要
High specific activity [H-3]BTCP, a radioligand for the dopamine-reuptake 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 [H-3]BTCP in 7.3% yield with a specific activity of 29.8 Ci/mmol (51.4% isotopic incorporation).
引用
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页码:165 / 173
页数:9
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