With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.399-51-9,6-Fluoro-1H-indole,as a common compound, the synthetic route is as follows.
A 250 L reactor was charged with approx. 40% aq. dimethylamine (35.7 kg, 317 mol) at approx. 17C. under an inert atmosphere. The mixture was cooled to approx. 4.5 C. and glacial acetic acid (43.4kg, 723 mol) was added dropwise over 140 mm while maintaining the temperature at approx. 15 C. Afier stirring for 20 mm at about 3 C., 37% aqueous formaldehyde (25.9 kg, 319 mol) was slowly added over about 20 mm while keeping the temperature between approx. 0C. to approx. 10C. 6-Fluoroindole (39.2kg, 290 mol) was added. The reaction was exothermic and reached a final temperature of approx. 40 C., and it was then cooled down to approx. 20 C. The reaction solution was slowly added to a 650 L reactor previously charged with aq. NaOH (3 M) over a period of approx. 40 mm. The formed suspension was stirred for approx. 40 mm while keeping the temperature between 5 to 20C. The precipitate was filtered from solution, washed with water on the filter, and dried at approx. 50 C. to afford Compound (II) (45.4 kg, 8 1%).
399-51-9, As the paragraph descriping shows that 399-51-9 is playing an increasingly important role.
Reference：
Patent; H. Lundbeck A/S; JACOBSEN, Mikkel Fog; NIELSEN, Ole; (16 pag.)US2016/168089; (2016); A1;,
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