Derivatives of 2-arylcyclopropylamine: Synthesis and interactions with 5-HT 1A receptors.

U Appelberg, N Mohell, U Hacksell

Index: Appelberg, Ulf; Mohell, Nina; Hacksell, Uli Bioorganic and Medicinal Chemistry Letters, 1996 , vol. 6, # 4 p. 415 - 420

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Citation Number: 6

Abstract

A series of cis-and trans-derivatives of2-aryl-N, N-dipropylcyclopropylamines and 1-(2- arylcyclopropyl)-N, N-dipropylmethylamines were synthesized and evaluated for affinity at the 5-HT1A receptor. The key step in the syntheses was a cyclopropanation of cis-and trans- 3-arylpropenoic esters with diazomethane which proceeds with retention of the stereochemistry. cis-1-[2-(3-Methoxyphenyl) cyclopropyl]-N, N-dipropylmethylamine (32) ...