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Synthesis of tritium labelled mecillinam

✍ Scribed by Søren Melsing Frederiksen; Gunnar Grue-Sørensen

Publisher: John Wiley and Sons
Year: 2003
Tongue: French
Weight: 96 KB
Volume: 46
Category: Article
ISSN: 0022-2135
DOI: 10.1002/jlcr.717

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✦ Synopsis

Abstract

The potent β‐lactam antibiotic mecillinam has successfully been labelled with tritium. 2,3,4,7‐Tetrahydro‐1H‐azepin‐1‐carbaldehyde was formed in a ring‐closing metathesis reaction and then condensed with trimethylsilyl protected penicillanic acid to give dehydro‐mecillinam. Pd/C catalysed tritiation then gave [^3^H~2~]‐mecillinam (6‐β (([3,4‐^3^H~2~]hexahydro‐1H‐azepin‐1‐yl)methyleneamino)penicillanic acid) with a radiochemical purity of 96% and a specific activity of 24 Ci/mmol. Copyright © 2003 John Wiley & Sons, Ltd.

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