Convenient procedures for synthesis of ciproxifan, a histamine H3-receptor antagonist.
Cyclopropyl 4-(3-(1H-imidazol-4-yl)propyloxy)phenyl methanone (ciproxifan) is a novel reference antagonist for the histamine H3 receptor. Despite the former Mitsunobu reaction the actual key reaction for preparation based on SNAr for acylated fluoroaromatics with an additional cyclization in a one-pot procedure needs no chromatographic purification steps and results in good yields.
Stark
H
H
Institut für Pharmazie, Freie Universität Berlin, Germany.
D006633:Histamine Antagonists / Q000138:chemical synthesis* / Q000737:chemistry; D007093:Imidazoles / Q000138:chemical synthesis* / Q000737:chemistry; D007202:Indicators and Reagents; D015394:Molecular Structure; D018100:Receptors, Histamine H3 / Q000187:drug effects*
D006633:Histamine Antagonists; D007093:Imidazoles; D007202:Indicators and Reagents; D018100:Receptors, Histamine H3; C115705:ciproxifan