Microwave-enhanced nucleophilic fluorination in the synthesis of fluoropyridyl derivatives of [3, 2-c] pyrazolo-corticosteroids, potential glucocorticoid receptor- …

…, E Konde, F Dossou, DC Labaree, RB Hochberg…

Index: Kahn, Michael G.C.; Konde, Emmanuel; Dossou, Francis; Labaree, David C.; Hochberg, Richard B.; Hoyte, Robert M. Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 13 p. 3454 - 3458

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Citation Number: 21

Abstract

Fluoropyridyl derivatives of [3, 2-c] pyrazolo-corticosteroids have high affinity for the glucocorticoid receptor (GR) and are highly active glucocorticoids. They are thus considered to be excellent candidates for PET imaging of GR containing tissues when labeled with fluorine-18 (t1/2= 110min). Previously reported syntheses of these fluorinated glucocorticoids were accomplished by conventional thermal nucleophilic halogen ...