The chemical development of selective and specific serotonin S2-antagonists was written by Kennis, Ludo E. J.;Vandenberk, Jan;Boey, Jozef M.;Mertens, Jos C.;Van Heertum, Albert H. M.;Janssen, Marcel;Awouters, Frans. And the article was included in Drug Development Research in 1986.Product Details of 58113-36-3 This article mentions the following:
Four types of chem. intermediates were prepared to synthesize novel piperidine derivatives as analogs of the butyrophenones benperidol and lenperone and the diphenylbutyl neuroleptic pimozide. The 1st type, comprising benzimidazolone alkyl intermediates, yielded declenperone [63388-37-4] and milenperone [59831-64-0] and also the sym. compound domperidone [57808-66-9], which was pharmacol. unusual by its specific peripheral dopamine antagonism. Declenperone was the most potent serotonin antagonist of that series, and replacement of the benzimidazolinonepropyl by the quinazolinedioneethyl moiety led to ketanserin [74050-98-9], which was devoid of residual dopamine antagonism. Very potent serotonin S2-antagonists were also obtained by using intermediates prepared from 2-aminoazaheterocycles. Pirenperone [75444-65-4] and setoperone [86487-64-1] had a complex pharmacol. profile, including dopamine and norepinephrine antagonism. These activity components were absent from the profile of R 56413 [87071-17-8] and ritanserin [87051-43-2], which were obtained by using the 4th intermediate, benzhydrylenepiperidine. R 56413 and ritanserin are the most specific of the presently known serotonin S2-antagonists. Some structure-activity relations with respect to the different pharmacophores examined are discussed. In the experiment, the researchers used many compounds, for example, 4-(Bis(4-fluorophenyl)methylene)piperidine (cas: 58113-36-3Product Details of 58113-36-3).
4-(Bis(4-fluorophenyl)methylene)piperidine (cas: 58113-36-3) belongs to piperidine derivatives. Piperidine and its derivatives have become increasingly popular in many synthetic schemes. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Product Details of 58113-36-3
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem