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2-METHYLQUINOLINE-3,4-DICARBOXYLIC ACID synthesis

3synthesis methods
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Yield:88344-65-4 91.6%

Reaction Conditions:

Stage #1: indole-2,3-dionewith water;sodium hydroxide at 20; for 1 h;
Stage #2: acetoacetic acid methyl ester for 12 h;

Steps:

1 [Production Example 1: Preparation of Compound A]

In a 500ml beaker, add isatin (7.36g, 50mmol, 1.0eq) and 150ml of 25% NaOH aqueous solution. After stirring at room temperature for 1 hour, methyl acetoacetate (11.6g, 100mol, 2.0eq) was added and stirred for 12 hours. Then a white solid was formed. When the reaction was completed, 175 ml of a 10% HCl aqueous solution was slowly added, stirred, and filtered. After washing with a little water and drying in a vacuum oven (oven) at 60°C compound [A] (10.6g, 45.8mmol, 91.6%) was obtained.

References:

KR2021/39113,2021,A Location in patent:Paragraph 0179-0182

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