C. Haubmann et al., Piperidinylpyrroles: Design, synthesis and binding properties of novel andselective dopamine D4 receptor ligands, BIOORG MED, 9(21), 1999, pp. 3143-3146
Piperidinylpyrroles of type 3 were synthesized through a modified Paal-Knor
r reaction. For the introduction of pyrrole-substituents high yielding tran
sformations including Sonogashira cross-coupling reactions were utilized. E
mployment of the reagent TosMIC gave access to the regioisomeric oxazolyl d
erivatives 7 and 11 which showed the highest dopamine D4 receptor binding o
f the series investigated. (C) 1999 Elsevier Science Ltd. All rights reserv
ed.