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Synthesis of carbon-14 labelled midazolam

✍ Scribed by John A. Easter; Richard C. Burrell; Samuel J. Bonacorsi Jr; Balu Balasubramanian

Publisher
John Wiley and Sons
Year
2009
Tongue
French
Weight
88 KB
Volume
52
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

Cytochrome P450 (CYP) enzymes are responsible for much of the phase I oxidative metabolism observed in vivo. Many important pharmaceutical compounds are metabolized by CYP. Co‐administration of a drug with another agent can alter the efficacy or the toxicity, especially in cases where drug clearance depends primarily on the CYP metabolism. Compounds that induce or inhibit the CYP activity are often used in drug–drug interaction studies. Midazolam is one such compound that is routinely used in drug–drug interaction studies because it is a known substrate for CYP3A enzymes. The synthesis of this important tool molecule has been documented, but unfortunately a detailed preparation of carbon‐14‐labelled midazolam has not been reported in the literature. This paper describes a two‐step synthesis leading to [^14^C]midazolam. A total of 4.5 mCi of [^14^C]midazolam was obtained having a specific activity of 120.1 µCi/mg (39.12 mCi/mmol). The radiochemical purity as determined by HPLC was 99.8% and the overall radiochemical yield was 9%. Copyright © 2009 John Wiley & Sons, Ltd.

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