Please use this identifier to cite or link to this item:
|Type:||Artigo de periódico|
|Title:||Heck Arylations Of N-acyl-3-pyrroline And N-acyl-1,2,5,6-tetrahydropyridine With Aryldiazonium Salts. Short Syntheses Of Aryl γ- And δ-lactams, Baclofen, Homobaclofen And Analogues|
|Abstract:||Heck arylation of N-acyl-3-pyrrolines and an N-acyl-tetrahydropyridine with aryldiazonium tetrafluoroborates under phosphine-free conditions proceeded smoothly to give α-hydroxycarbamates (hemiaminals) or α-alkoxycarbamates which were oxidized to the desired γ- and δ-lactams. Acidic hydrolysis of the γ-lactams produced a series of arylated GABA derivatives, including baclofen, a useful therapeutic drug, in only three steps with an overall yield of 63-76%. Starting from N-acyl-tetrahydropyridine, aryl-δ-lactams and higher homologues of baclofen can be obtained. © 2002 Elsevier Science Ltd. All rights reserved.|
|Appears in Collections:||Unicamp - Artigos e Outros Documentos|
Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.