These common heterocyclic compound, 98446-49-2, name is 2,4-Dichloro-5-methoxyaniline, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route. category: chlorides-buliding-blocks
Cyanoacetic acid (50 g) was added to ethyl acetate (400 mL) at 25 C followed by addition of dimethylformamide (2 mL). The obtained reaction mixture was cooled to 0C and oxalyl chloride (82.6 g) was slowly added at 0C to 5C over a period of about 60 minutes. The temperature of the reaction mixture was raised up to 25C to 28C and stirred for 2 hours. 2,4-dichloro-5-methoxyaniline (100 g, obtained from Step-3) was added to the reaction mixture and heated up to 55C to 60C under stirring for about 2 hours. Deionized water (200 mL) was added to the reaction mixture at 20C to 30C followed by stirring for 1 hour. The product obtained was filtered and washed with ethyl acetate (50 mL) followed by deionized water (500 mL) and ethyl acetate (200 mL) respectively. The wet product was dried in air oven to provide the title product. Yield: 97 g Chromatographic Purity: 99.67%
The synthetic route of 2,4-Dichloro-5-methoxyaniline has been constantly updated, and we look forward to future research findings.
Reference:
Patent; SUN PHARMACEUTICAL INDUSTRIES LIMITED; HANDIQUE, Sourav; KUMAR, Ashok; GOTTIPAMULA, Narender; JAIN, Amit Kumar; PRASAD, Mohan; SINGH, Kaptan; (10 pag.)WO2019/186429; (2019); A1;,
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