57257-41-7Relevant academic research and scientific papers
Synthesis of terfenadine
Carr,Meyer
, p. 1157 - 1159 (2007/10/02)
The synthesis of α-[4-(1,1-dimethylethyl)phenyl]-4-(hydroxydiphenylmethyl)-1-piperidinebut anol (terfenadine, RMI 9918, Triludan, Teldane, resp.) is described. A limited structure-activity analysis of the central nervous system-mediated side effects of this compound and related analogs is made relative to the antipsychotic agent, haloperidol. Modification of the piperidine 4-position substituents of haloperidol to give a 4-(α,α-diphenylmethyanol) moiety has conveyed histamine H1-antagonism to the antipsychotic agent, haloperidol. Structural changes of this fluorobutyrophenone have progressively reduced and finally eliminated centrally-mediated side effects. The result of this exercise is terfenadine, a preferred antihistamine, potent and selective in antagonizing histamine H1-receptor-mediated responses but lacking the usual side effect profile of known histamine H1-receptor antagonists.
Substituted piperidine derivatives
-
, (2008/06/13)
Novel compounds useful as antihistamine agents, antiallergy agents, and bronchodilators are represented by the following formula SPC1 Wherein R1 represents cyclohexyl, phenyl, or substituted phenyl wherein the substituent on the substituted phe
