Preparation of Conformationally Constrained α2 Antagonists: The Bicyclo [3.1. 0] hexane Approach

B Bonnaud, P Funes, N Jubault…

Index: Bonnaud, Bernard; Funes, Philippe; Jubault, Nathalie; Vacher, Bernard European Journal of Organic Chemistry, 2005 , # 15 p. 3360 - 3369

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Citation Number: 10

Abstract

Abstract The aim of the research was to discover antagonists at α 2 receptor subtypes potentially more selective than known compounds. We focused on new, conformationally restricted analogues of atipamezole. The key step in the synthetic sequences leading to target compounds relied on a rhodium-catalyzed intramolecular cyclopropanation reaction, the outcome of which varied with the nature of the diazo styrene precursor. Thus, ...