Analyzing the synthesis route of 399-51-9

399-51-9 6-Fluoro-1H-indole 351278, aindole-building-block compound, is more and more widely used in various fields.

399-51-9, 6-Fluoro-1H-indole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Procedure Using Formaldehyde in Place of Diethoxymethane:To a 250 L reactor, under N2 atmosphere, was charged with about 40% aqueous dimethylamine (35.68 kg, 1.0 eqv.) at about 17 C. The mixture was cooled to about 4.5 C. and glacial acetic acid (43.4 kg, 2.5 eq.) was added dropwise over 140 min while maintaining the temperature using below about 15 C. After stirring for 20 min at about 3 C., 37% aqueous formaldehyde (25.9 kg, 1.1 eq.) was slowly added over about 20 min while keeping the temperature between about 0 C. to about 10 C. 6-Fluoroindole (39.2 kg) was added. The reaction was exothermic and reached a final temperature of about 40 C., which was then cooled down to about 20 C. The reaction solution was slowly added in a 650 L reactor charged with aqueous 3M NaOH over a period of about 40 min. The suspension was stirred for about 40 min while keeping the temperature between about 5 and 20 C. The product was filtered, rinsed with DI water (120 kg) and dried at about 50 C. to afford the compound of Formula II (45.4 kg). Yield: 85%., 399-51-9

399-51-9 6-Fluoro-1H-indole 351278, aindole-building-block compound, is more and more widely used in various fields.

Reference:
Patent; H. LUNDBECK A/S; US2011/152539; (2011); A1;,
Indole alkaloid derivatives as building blocks of natural products from?Bacillus thuringiensis?and?Bacillus velezensis?and their antibacterial and antifungal activity study
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles