Hydrochloric Acid → (4-Fluoro-benzylamino)-phenyl-acetic acid hydrochloride

関与物質

反応手順

4-Fluorobenzaldehyde (0.25 mL, 2.38 mmol), 2-amino-2-phenylacetic acid (300 mg, 1.98 mmol) and NaOH (79 mg, 1.98 mmol) are dissolved in MeOH (20 mL) and stirred at RT overnight. The reaction is cooled at 0° C. and NaBH4 (150 mg, 3.97 mmol) is added. After being stirred at 0° C. for 30 minutes, the reaction is judged complete by UPLC-MS analysis. 4M HCl in dioxane is added dropwise till pH 5 and the precipitate is collected by suction filtration, washed with Et2O and dried under vacuum at 40° C. to obtain intermediate I129 as a white solid (587 mg, quantitative yield).

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