Premium
Convenient Procedures for Synthesis of Ciproxifan, a Histamine H 3 ‐Receptor Antagonist
Author(s) -
Stark Holger
Publication year - 2000
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/1521-4184(20009)333:9<315::aid-ardp315>3.0.co;2-m
Subject(s) - chemistry , antagonist , histamine , histamine h3 receptor , competitive antagonist , combinatorial chemistry , stereochemistry , pharmacology , receptor , biochemistry , medicine
Cyclopropyl 4‐(3‐(1 H ‐imidazol‐4‐yl)propyloxy)phenyl methanone (ciproxifan) is a novel reference antagonist for the histamine H 3 receptor. Despite the former Mitsunobu reaction the actual key reaction for preparation based on S N Ar for acylated fluoroaromatics with an additional cyclization in a one‐pot procedure needs no chromatographic purification steps and results in good yields.