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Carbon-11 labeling of a potent, nonpeptide, at1-selective angiotensin-II receptor antagonist: MK-996

✍ Scribed by William B. Mathews; H. Donald Burns; Robert F. Dannals; Hayden T. Ravert; Elizabeth M. Naylor

Publisher
John Wiley and Sons
Year
1995
Tongue
French
Weight
415 KB
Volume
36
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

[α‐^11^C]Benzoyl chloride was synthesized and purified by normal phase HPLC. [^11^C]MK‐996 ([^11^C]N‐[[4′[(2‐ethyl‐5,7‐dimethyl‐3H‐imidazo [4,5‐b]pyridin‐3‐yl)methyl][1,1′‐biphenyl]‐2‐yl]sulfonyl]‐benzamide), a potent and selective ligand for the AT~1~ receptor, was prepared by N‐benzoylation of L‐159,221 with [α‐^11^C]benzoyl chloride in tetrahydrofuran using lithium bis(trimethylsilyl)amide as a base. The radiotracer was purified by semi‐preparative reverse‐phase HPLC. The average specific activity was 1162 mCi/μmol calculated at end‐of‐synthesis (EOS). The average time of synthesis including formulation was 30 minutes.

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