Solid-phase synthesis of libraries generated from a 4-phenyl-2-carboxy-piperazine scaffold.
Strategies for finding novel structures of therapeutical interest are discussed. The rationale for the selection of the two scaffolds N4-(m-aminophenyl)-piperazine-2-carboxylic acid E and N4-(o-aminophenyl)-piperazine-2-carboxylic F is described. The synthesis of the appropriate precursors to scaffold E and F and their use in solid-phase chemistry are described. A 160-member library was produced combining these novel piperazine scaffolds with eight sulfonyl chlorides/acid chlorides and 10 amines. The compound library prepared was analyzed using LC-MS, showing the expected base peak in all wells at an average purity of 82%.
Nilsson
J W
JW
Department of Chemistry, Linköping University, S-581 83 Linköping, Sweden.
Thorstensson
F
F
Kvarnström
I
I
Oprea
T
T
Samuelsson
B
B
Nilsson
I
I
D002121:Calcium Channel Blockers / Q000138:chemical synthesis; D002626:Chemistry, Pharmaceutical; D020650:Combinatorial Chemistry Techniques; D004095:Dihydropyridines / Q000737:chemistry; D010879:Piperazines / Q000737:chemistry*; D013329:Structure-Activity Relationship
C450001:4-phenyl-2-carboxy-piperazine; D002121:Calcium Channel Blockers; D004095:Dihydropyridines; D010879:Piperazines