3-AMINO-3-(3,5-DIFLUORO-PHENYL)-PROPIONIC ACID synthesis
- Product Name:3-AMINO-3-(3,5-DIFLUORO-PHENYL)-PROPIONIC ACID
- CAS Number:682804-73-5
- Molecular formula:C9H9F2NO2
- Molecular Weight:201.17
141-82-2
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Yield:682804-73-5 56%
Reaction Conditions:
with ammonium acetate in ethanol;Reflux;
Steps:
The mixture of 3, 5-difluorobenzylaldehyde (S1) (27.09 g, 0.19 mol, 1.0 equiv.), malonic acid (19.84 g, 0.19 mol, 1.0 equiv.), and ammonium acetate (29.39 g, 0.38 mol, 2.0 equiv.) in ethanol (300 mL) was stirred under reflux overnight. The white precipitate was filtered, rinsed with cold ethanol, dried under vacuum, and compound S2 was obtained (21.28 g, 0.11mol, 56% yield). 1H NMR (CD3OD): δ: 7.18-7.05 (m, 2 H); 7.00-6.95 (m, 1H), 4.53 (t, J = 7.0 Hz, 1H), 2.66 (d, J = 7.2 Hz, 2H). Electrospray MS: Obs. [M+H]: 202.1.
References:
WO2010/56722,2010,A1 Location in patent:Page/Page column 334