A series of bisaryl imidazolidin-2-ones has shown to be selective and orally active 5-HT2C receptor antagonists
Bisaryl cyclic ureas have been identified as high affinity 5-HT 2C receptor antagonists with selectivity over 5-HT2A and 5-HT2B. Compounds such as 8 and 22 have shown oral activity in a centrally mediated pharmacodynamic model of 5-HT2C function in rodents.
Goodacre, Caroline J.,Bromidge, Steven M.,Clapham, David,King, Frank D.,Lovell, Peter J.,Allen, Mike,Campbell, Lorraine P.,Holland, Vicky,Riley, Graham J.,Starr, Kathryn R.,Trail, Brenda K.,Wood, Martyn D.
p. 4989 - 4993
(2007/10/03)
Alkoxide-Accelerated Smiles Rearrangements. Synthesis of N-(2-Hydroxyethyl)anilines from N-(2-Hydroxyethyl)(aryloxy)acetamides
The first example of an alkoxide-accelerated Smiles rearrangement is reported.The rearrangement of N-(2-hydroxyethyl)(aryloxy)acetamides in dimethylformamide or tetrahydrofuran-18-crown-6 and potassium hydride produces useful yields of substituted N-(2-hydroxyethyl)anilines.
Baker, William R.
p. 5140 - 5143
(2007/10/02)
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