(4-Chloro-2-fluorophenyl)(cyclopropyl)methanol synthesis

Yield:-

Reaction Conditions:

in tetrahydrofuran at -70 - 25; for 2 h;

Steps:

1.1 Step 1: Synthesis of compound 2-2

2-1 (5.0 g, 31.53 mmol) and tetrahydrofuran (50 mL) were added to a reaction flask. The reaction mixture was cooled to -70 °C, and cyclopropylmagnesium bromide (0.5 M, 151.36 mL) was added. The resulting mixture was continued to stir at -70 °C for 1 hour, then slowly warmed to 25 °C, and stirred at 25 °C for 1 hour. To the reaction mixture was added saturated ammonium chloride aqueous solution (200 mL), and the mixture was extracted with ethyl acetate (200 mL×3); the organic phases were combined, dried over anhydrous sodium sulfate, and concentrated under reduced pressure to obtain 2-2. MS m/z: 183 [M-17]⁺.

References:

EP4043450,2022,A1 Location in patent:Paragraph 0135-0136