Optimization studies concerning the direct nucleophilic fluorination of butyrophenone neuroleptics
✍ Scribed by A. Katsifis; K. Hamacher; J. Schnitter; G. Stöcklin
- Book ID
- 103989127
- Publisher
- Elsevier Science
- Year
- 1993
- Tongue
- English
- Weight
- 506 KB
- Volume
- 44
- Category
- Article
- ISSN
- 0969-8043
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✦ Synopsis
Based on the direct nucleophilic aromatic substitution described previously for ["FIN-methylspiperone the butyrophenone neuroleptics benperidol, droperidol, fluanisone and haloperidol were labelled with fluorine-18. The n.c.a. aromatic nucleophilic NO]-+ "F substitution takes place in the presence of the moderately basic cryptate system consisting of Kryptofix K 2.2.2., potassium oxalate and potassium carbonate. The one step labeling reaction was performed in different solvents and is equally successful in dimethylsulfoxide, dimethylformamide or dimethylacetamide yielding 25535% (EOS) within a reaction time of 5530 min in the range of 140-160°C at analytical activity levels.