Downstream synthetic route of 247037-82-7

The synthetic route of 247037-82-7 has been constantly updated, and we look forward to future research findings.

247037-82-7, Thiazole-2-carboximidamide hydrochloride is a thiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A 1000 L glass-lined reactor equipped with mechanical stirrer, thermometer and nitrogen bubbler was charged 2-chloro-4-fluoro-benzaldehyde (30.8 kg, 194 mol, compound 11-a) andIPA (188.0 kg). To the solution was then added methyl acetoacetate (22.7 kg, 195 mol, compound 11-b) followed by addition of piperidine (1.74 kg, 20.4 mol) and acetic acid (1.32 kg, 22.0 mol). The reaction mixture was then heated to 43 C-47 C and stirred at such temperature for 5 hours. Then to the reaction mixture was added thiazole-2-carboxamidine hydrochloride salt (19.8 kg, 121.0 mol, compound 8-c) followed by addition of triethylamine (20.0 kg, 198.0 mol).The reaction mixture was heated to 80 C – 85 C and stirred for 7 hours. After reaction was completed, the reaction mixture was cooled to 20 C-25 C and then added water (52.0 kg). The resulting suspension was stirred at 20 C-25 C for 2 hours. The solid was collected by centrifuge and washed with isopropanollwater (42 kg, v/v=10/3). The wet solid was dried in vacuum oven to afford Example 11 (35.05 kg, purity: 95.8%, Yield: 79.2%) as yellow solid. MS mle = 366.2[M+H] .

The synthetic route of 247037-82-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; CHEN, Junli; (58 pag.)WO2017/140750; (2017); A1;,
Thiazole | C3H3NS – PubChem
Thiazole | chemical compound | Britannica