Regioselective Preparation of 3??Alkoxy??4, 5??difluoroanilines by SNAr

…, C Martínez??Lamenca, J Leenaerts…

Index: Van Brandt, Sven; Rombouts, Frederik J. R.; Martinez-Lamenca, Carolina; Leenaerts, Jos; Rauws, Tom R. M.; Trabanco, Andres A. European Journal of Organic Chemistry, 2012 , # 36 p. 7048 - 7052

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Abstract

Abstract A simple and scalable procedure to introduce alcohols selectively at the 3-position of 3, 4, 5-trifluoroaniline is described. The procedure uses powdered NaOH as base and catalytic 15-crown-5 in refluxing toluene with a Dean–Stark trap. A short exploration of other nucleophiles and fluoroaryl electrophiles is also described.

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