Novel synthesis of 2-[18F]-fluoroisonicotinic acid hydrazide and initial biological evaluation
| Autor: | J.K. Amartey, B. Al-Otaibi, I. Al-Jammaz, C. Esguerra |
|---|---|
| Rok vydání: | 2002 |
| Předmět: |
Cancer Research
Biodistribution Metabolic Clearance Rate Hydrazine Hydrazide Mice chemistry.chemical_compound Nucleophile Reference Values Animals Tuberculosis Organic chemistry Tissue Distribution Radiology Nuclear Medicine and imaging Radiometry Radionuclide Imaging Acetonitrile Cells Cultured Total synthesis Hydrazines Streptococcus pneumoniae chemistry Organ Specificity Yield (chemistry) Mice Inbred CBA Feasibility Studies Molecular Medicine Female Isonicotinic Acids Radiopharmaceuticals Phase-transfer catalyst Nuclear chemistry |
| Zdroj: | Nuclear Medicine and Biology. 29:817-823 |
| ISSN: | 0969-8051 |
| DOI: | 10.1016/s0969-8051(02)00340-2 |
| Popis: | 2-[18F]-Fluoroisonicotinic acid hydrazide was synthesized by nucleophilic displacement reaction on ethyl-2- (trimethylammonium)-isonicotinate precursor in acetonitrile. Kryptofix 222 was used as the phase transfer catalyst. The intermediate fluorinated ethyl ester reacted with hydrazine hydrate to produce the hydrazide in excellent radiochemical yield. The overall radiochemical yield was greater than 70% with total synthesis time of approximately 60 minutes. Biological evaluation was performed in bacterial cells and biodistribution in normal CBA/J mice. It was found that the S. pneumoniae cells retained the radiotracer in an in vitro assay. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full Text from ScienceDirect