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Solid-phase synthesis of libraries generated from a 4-phenyl-2-carboxy-piperazine scaffold.

Domenii publicaţii > Chimie + Tipuri publicaţii > Articol în revistã ştiinţificã

Autori: Nilsson, Jonas W.; Thorstensson, Fredrik; Kvarnstroem, Ingemar; Oprea, Tudor I.; Samuelsson, Bertil; Nilsson, Ingemar.

Editorial: Journal of Combinatorial Chemistry, 3(6), p.546-553, 2001.


Strategies for finding novel structures of therapeutic interest are discussed. The rationale for the selection of the two scaffolds N-4-(m-aminophenyl)-piperazine-2-carboxylic acid (I) and N-4-(o-aminophenyl)-piperazine-2-carboxylic (II) is described. The synthesis of the appropriate precursors to scaffold I and II and their use in solid-phase chem. are described. A 160-member library was produced combining these novel piperazine scaffolds with eight sulfonyl chlorides/acid chlorides and 10 amines. The compd. library prepd. was analyzed using LC-MS, showing the expected base peak in all wells at an av. purity of 82%.

Cuvinte cheie: Combinatorial chemistry, Solid-phase synthesis, Lead-like library, Phenylcarboxypiperazine scaffold