4-amino-5-chloro-2-fluorobenzoic acid synthesis

2synthesis methods

Product Name:4-amino-5-chloro-2-fluorobenzoic acid
CAS Number:1001346-86-6
Molecular formula:C7H5ClFNO2
Molecular Weight:189.57

Benzoic acid, 4-amino-5-chloro-2-fluoro-, 1,1-dimethylethyl ester

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Yield:1001346-86-6 100%

Reaction Conditions:

with trifluoroacetic acid in dichloromethane at 18 - 25; for 1 h;

Steps:

4-Amino-5-chloro-2-fluorobenzoic acid tert-butyl ester (Intermediate 50; 3.0 g, 12.21 mmol) was dissolved in DCM (75 mL) and trifluoroacetic acid (25 niL) added. The mixture was stirred for 1 hour at room temperature and then concentrated to yield the title compound as a pale yellow solid (2.45 g, 100%).¹H NMR (399.9 MHz₅ DMSOd₆) 66.40 (2H₅ s), 6.53 - 6.56 (IH, m), 7.67 (IH, d), 12.56 (IH, s).

References:

WO2008/40951,2008,A1 Location in patent:Page/Page column 164

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References