Two series of 1-phenylpiperazinylpropyl derivatives 10, 11, 16, 17 and 19-24, structurally related to previously described 5-HT1A or 5-HT2A ligands 4 and 1, respectively, were synthesized and their binding properties were determined. Structural modifications which involved 1,3-diazepine ring opening in 4 (compounds 10, 11, 15, 16) and replacement of spiroalkyl moiety in 1 by aryl substituent (19-24) did not improve binding affinity and selectivity of the tested compounds. The results showed, however, that the diazepine ring present in 4 or spiroalkyl ring in 1 are important for high 5-HT1A or 5-HT2A binding affinity and selectivity of these compounds. (C) 2000 Elsevier Science S.A. All rights reserved.
Microwave-enhanced rhodium-catalyzed conjugate-addition of aryl boronic acids to unprotected maleimides
作者:Pravin S. Iyer、Meaghan M. O’Malley、Matthew C. Lucas
DOI:10.1016/j.tetlet.2007.04.084
日期:2007.6
Various boronicacids were treated with a rhodium (I) catalyst enabling their 1,4-conjugate addition to unprotected maleimide. The scope of the reaction was explored to include both electron-rich and electron poor boronicacids. These reactions were also performed in the microwave resulting in reduced reaction times and improved efficiencies. Additionally, substrates that were recalcitrant under conventional