Abstract
An analogue of RP 62203 having radioiodine in the 4-position of the 1,8-naphthosultam ring system has been prepared for evaluation as a ligand for the serotonin 5-HT(2A) receptor. Non-radioactive 4-iodo-RP 62203 was synthesized in three steps (20% overall yield) by iodination of 1,8-naphthosultam with iodine monochloride followed by N-alkylation with 1-bromo-3-chloropropane and coupling with 1-(4-fluorophenyl)piperazine. The precursor for radiolabeling was prepared in 83% yield from 4-iodo-RP 62203 and hexamethylditin by palladium-mediated trimethylstannylation. Electrophilic radioiododestannylation gave 4-[125I]-Rp 62203 in good isolated yield (80-86%), with high purity (≤ 99.6%) and specific radioactivity (1200-2066 mCi/CLmol).
Original language | English (US) |
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Pages (from-to) | 143-150 |
Number of pages | 8 |
Journal | Journal of Labelled Compounds and Radiopharmaceuticals |
Volume | 41 |
Issue number | 2 |
DOIs | |
State | Published - Feb 1998 |
Externally published | Yes |
Keywords
- RP 62203
- Radioiodine
- Serotonin receptor
ASJC Scopus subject areas
- Analytical Chemistry
- Biochemistry
- Radiology Nuclear Medicine and imaging
- Drug Discovery
- Spectroscopy
- Organic Chemistry