| |
[摘要]：The suitably protected precursors for direct fluorination, N-b-Boc di-protected 5-fluorotryptamine (13), N-b-acetyl-N-b-Boc protected 5-halotryptamines (15a-c), were treated with Selectfluor (TM) in MeCN/water in the presence of NaHCO3 to give the corresponding 3-fluorooxindoles 14 and 16a-c in good yields. Removal of the protecting groups of 14 and 16a-c produced (3,5-difluorooxindol-3-yl)ethylamine (8) and N-acetyl-(3-fluoro-5-halooxindol-3-yl)ethylamines (9a-c) in excellent yields, respectively. These compounds are potentially non-epimerizable analogs for the putative metabolites of 5-fluorotryptamine (6) and N-b-acetyl-5-halotryptamines (7a-c). |
|
