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ChemicalBook CAS DataBase List 2-Fluorophenylboronic acid
1993-03-9

2-Fluorophenylboronic acid synthesis

10synthesis methods
-

Yield:1993-03-9 85%

Reaction Conditions:

Stage #1: o-fluorobromobenzenewith n-butyllithium in tetrahydrofuran at -70; for 0.5 h;Inert atmosphere;Autoclave;Large scale;
Stage #2: Triisopropyl borate in tetrahydrofuran at -70;Large scale;

Steps:

1 Example 1 Preparation of Compound 2

Under nitrogen atmosphere, 14 kg (22.9 mol) of the compound and 20 L of THF were sequentially added to the 50 L autoclave, and the temperature was lowered to -70 ° C.Temperature control -70 the following dropping n-BuLi6.8kg, after dropping at -70 below stirring 0.5 hours. Temperature -70 below the dropBoric acid isopropyl ester 4.75kg, drop back after the natural warm night. Poured into 20L (1N) dilute hydrochloric acid, liquid, water phase and thenEA10L. The combined organic phases were washed once with saturated brine 10 L, dried over anhydrous sodium sulfate, filtered and concentratedTo give 22.4 kg of the compound in 85% yield.

References:

CN105801553,2016,A Location in patent:Paragraph 0093; 0094; 0095

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