2-(3-Trifluoromethylphenyl)glycine hydrochloride is a precursor of substituted 2-acetamido-5-aryl-l, 2,4-triazolones. Substituted 2-acetamido-5-aryl-l, 2,4-triazolones are dual V1a/V2 receptor antagonists and can be used in cardiovascular disease research[1].
Synthesis
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Example 95A: Synthesis of 2-amino-2-(3-trifluoromethylphenyl)acetic acid hydrochloride
1.00 g (3.13 mmol) of N-tert-butoxycarbonyl-2-(3-trifluoromethylphenyl)-DL-glycine was mixed with 15.7 mL of a dioxane solution of 4N HCl and stirred overnight at room temperature. Upon completion of the reaction, the volatile components were removed using a rotary evaporator. The residue was dried under high vacuum (HV) to give 795 mg (99% of theoretical yield) of 2-amino-2-(3-trifluoromethylphenyl)acetic acid hydrochloride.LC/MS [Method 2]: rt = 0.79 min; m/z = 220 (M + H)+.
References
[1] Ulf Brüggemeier, et al. Substituted 2-acetamido-5-aryl-1,2,4-triazolones and use thereof. WO2010105770A1
