625389-73-3Relevant academic research and scientific papers
Synthesis of 1-arylpiperazyl-2-phenylcyclopropanes designed as antidopaminergic agents: Cyclopropane-based conformationally restricted analogs of haloperidol
Yamaguchi, Kazuya,Kazuta, Yuji,Hirano, Kazufumi,Yamada, Shizuo,Matsuda, Akira,Shuto, Satoshi
experimental part, p. 8875 - 8881 (2009/04/11)
A series of the cyclopropane-based conformationally restricted analogs of haloperidol were designed as potential antidopaminergic agents and were effectively synthesized using highly stereoselective Grignard reaction with tert-butanesulfinyl imines as the key step. Pharmacological evaluation of the compounds showed that the conformational restriction method can effectively work for improving the pharmacological selectivity of a parent compound and also for investigating the bioactive conformation.
Construction of a cis-Cyclopropane via Reductive Radical Decarboxylation. Enantioselective Synthesis of cis- and trans-1-Arylpiperazyl-2-phenylcyclopropanes Designed as Antidopaminergic Agents
Yamaguchi, Kazuya,Kazuta, Yuji,Abe, Hiroshi,Matsuda, Akira,Shuto, Satoshi
, p. 9255 - 9262 (2007/10/03)
(1S,2S)-, (1S,2R)-, and (1R,2S)-1-(2,4-Dimethylphenyl)piperazyl-2-phenylcyclopropane (2a, 3, and ent-3, respectively), which were designed as conformationally restricted analogues of haloperidol (1), a clinically effective antipsychotic agent, were synthe
