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Side-chain modified analogues of histaprodifen: Asymmetric synthesis and histamine H₁-receptor activity

Patil, Rameshwar ; Elz, Sigurd ; Reiser, Oliver



Abstract

New analogues of histaprodifen with polar side chains have been stereo selectively synthesized and evaluated as histamine H-1-receptor agonists. As a key transformation the asymmetric aminohydroxylation has been used, which was successfully realized for the first time on an imidazolyl derivative. While all chiral analogues proved to be weak H-1-receptor antagonists, an achiral keto derivative of ...

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