5-Amino-2-fluorophenylacetic acid 98%

To a suspension of 2-(2-fluoro-5-nitrophenyl)acetic acid (15.0 g, 75.3mmol) in ethanol (80OmL), THF (40OmL), and water (20OmL) was added ammonium chloride (4.46 g, 83.4mmol) and ferrous powder (25.04 g, 405.4mmol). The resulting mixture was heated at 80 a. 2-(5-Amino-2-fluoro-phenyl)-ethanol (Intermediate Ya) Borane-THF complex (1M, 11.8 mL, 11.8 mmol) was added to a solution of Borane-THF complex (1M, 11.8 mL, 11.8 mmol) was added to a solution of (5- amino-2-fluoro-phenyl)-acetic acid (1.00 g, 5.91 mmol) in dry THF (10 mL), under argon, over 20 min. Once the effervescence had ceased, the reaction mixture was heated to 50 C for 2 h. The mixture was left to cool and then concentrated in vacuo. The residue was re-dissolved in DCM (25 mL) and treated with MeOH (2 mL). The mixture was stirred vigorously and then concentrated in vacuo. The residue was dissolved in MeOH (25 mL) and re-concentrated in vacuo. The residue was purified by FCC, using 0-10% [2M NH3 in MeOH] in DCM, to afford the title compound (0.54 g, 59%). LCMS (Method 3): Rt: 0.41 min, m/z 156 [MH+].General procedure: To a stirred solution of 9a (130 mg, 0.7 mmol) in EtOAc (10 mL) was added dropwise a solution of CH2N2 in ether until bubbling ceased. The reaction mixture was concentrated in vacuo to yield 10a (146 mg, quant) as a pale yellow oil;To a suspension of 2-(2-fluoro-5-nitrophenyl)acetic acid (15.0 g, 75.3mmol) in ethanol (80OmL), THF (40OmL), and water (20OmL) was added ammonium chloride (4.46 g, 83.4mmol) and ferrous powder (25.04 g, 405.4mmol). The resulting mixture was heated at 80 0C for 1 hr and the progress of the reaction was monitored by TLC. Upon complete consumption of starting material, the reaction mixture was filtered off while it was hot. The filtrate was evaporated under vacuum and the crude residue was diluted with ethyl acetate (20OmL) and washed with water (3 x 10OmL). The combined organic layer was washed with brine, dried over Na2SO4 and evaporated under vacuum to afford 2-

Molecular Weight:169.15
XLogP3:0.8
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:4
Rotatable Bond Count:2
Exact Mass:169.05390666
Monoisotopic Mass:169.05390666
Topological Polar Surface Area:63.3
Heavy Atom Count:12
Complexity:174
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes