A concise and efficient synthesis of flumazenil and its precursor for radiolabeling with fluorine-18

SR Donohue, RF Dannals

Index: Donohue, Sean R.; Dannals, Robert F. Tetrahedron Letters, 2009 , vol. 50, # 52 p. 7271 - 7273

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Citation Number: 11

Abstract

Presently there is a strong interest in developing radioligands for in vivo imaging the GABAA- Bz site with positron emission tomography (PET). Flumazenil (1), a high-affinity GABAA-Bz site inverse agonist, is amenable for 11C and 18F-labeling. The current methods for synthesis of 1 and its precursor for 18F-labeling are not ideal and restrict structure–activity relationship (SAR) development. Herein we present a novel and less troublesome ...