Journal of medicinal chemistry

Synthesis of high specific activity [75Br]-and [77Br] Bromperidol and tissue distribution studies in the rat

SM Moerlein, GL Stoecklin

Index: Moerlein, Stephen M.; Stoecklin, Gerhard L. Journal of Medicinal Chemistry, 1985 , vol. 28, # 9 p. 1319 - 1324

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Citation Number: 28

Abstract

A rapid synthesis of [75Br]-and [77Br] bromperidol with specific activity exceeding 10 000 Ci/mmol is described in which a trimethylstannylated analogue of bromperidol is used as a substrate for regiospecific no-carrier-added radiobromination. 4-[4-[4-(TrimethyLstannyl) phenyl]-4-hydroxypiperidino]-4'-fluorobutyrophenone was synthesized by the reaction of (trimethylstanny1) sodium with haloperidol and purified by preparative HPLC. Subsequent ...