Abstract
[α‐11C]Benzoyl chloride was synthesized and purified by normal phase HPLC. [11C]MK‐996 ([11C]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 AT1 receptor, was prepared by N‐benzoylation of L‐159,221 with [α‐11C]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.
Original language | English (US) |
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Pages (from-to) | 729-737 |
Number of pages | 9 |
Journal | Journal of Labelled Compounds and Radiopharmaceuticals |
Volume | 36 |
Issue number | 8 |
DOIs | |
State | Published - Aug 1995 |
Keywords
- Angiotensin
- Benzoyl chloride
- Carbon‐11
- PET
- Radiotracer
ASJC Scopus subject areas
- Analytical Chemistry
- Biochemistry
- Radiology Nuclear Medicine and imaging
- Drug Discovery
- Spectroscopy
- Organic Chemistry