methyl 3-amino-4-formylbenzoate synthesis

Yield:212322-17-3 94%

Reaction Conditions:

with water;acetic acid in ethanol at 20; for 0.333333 h;

Steps:

97.6

Step 6: 3-Amino-4-formyl-benzoic acid methyl ester (Compound 53); [0493] The product from the previous step (LOOMG, 0. 44MMOL) was dissolved at room temperature in a 15 mL solvent mixture composed of 2: 2: 1 EtOH- acetic acid-water. The strong yellow solution became pale yellow in 5 minutes. The mixture was let stand for an additional 15 minutes then was evaporated to dryness and was further dried in high vacuum overnight to get 75mg (94%) of the title intermediate as a yellow powder. [0494] H -NMR (CDCI3) : 6 (ppm) 9.92 (s, 1H, CHO), 7. 55 (d, 1H, Ar- H2), 7.34 (m, 2H, AR-H5+6), 3. 91 (s, 1H, CH3)

References:

WO2005/12288,2005,A1 Location in patent:Page/Page column 183