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1H-Indole-5-carboxylic acid, 2,3-diMethyl-, Methyl ester synthesis

3synthesis methods
-

Yield:21987-27-9 98%

Reaction Conditions:

with sulfuric acidReflux;

Steps:

6.2 Step 2. Synthesis of compounds 3.

To a solution of acid 2 (12.0 g, 63 mmol) in methanol (500 mL) conc. H2SO4 (50 mL) was added, and the resulted solution was refluxed overnight. The solvent was evaporated under reduced pressure. The residue was treated with NaHCO3 solution until the pH of the solution was reached 8-9. The mixture was extracted with EtOAc (3×50 mL), combined organic layers were dried over Na2SO4. After filtration the solution was concentrated under reduced pressure. The methyl ester 3 (12.7 g, 98%) was obtained as a colorless oil.

References:

WO2020/172565,2020,A1 Location in patent:Page/Page column 181; 182