Author/Authors :
Philippa A. Coates، نويسنده , , Peter Grundt، نويسنده , , Emma S. J. Robinson، نويسنده , , David J. Nutt، نويسنده , , Robin Tyacke، نويسنده , , Alan L. Hudson، نويسنده , , John W. Lewis، نويسنده , , Stephen M. Husbands، نويسنده ,
Abstract :
An irreversible ligand (7) has been prepared based on the selective I2 ligand 2-BFI. Compound 7 displayed high affinity and selectivity for I2-sites and has been shown to irreversibly bind to these sites in rat brain. Compound 7 should, therefore, prove an invaluable tool for the further elucidation of I2-site function.
Scheme 1. (a) BrCH(COOEt)2, K2CO3, Bu4NBr, toluene, reflux, 24 h, 84%. (b) NH3, EtOH, room temperature, 24 h, 99%. (c) POCl3, reflux, 0.5 h, 74%. (d) 1. HCl, MeOH, room temperature, 1 h; 2. ethylenediamine, reflux, 18 h, 52%. (e) Fe, HCl, EtOH, reflux, 3 h, 59%. (f) CSCl2, acetone–water, room temperature, 1.5 h, 75%.
