A new synthetic route of 866775-18-0

At the same time, in my other blogs, there are other synthetic methods of this type of compound,866775-18-0, Methyl 3-amino-6-bromo-5-(trifluoromethyl)picolinate, and friends who are interested can also refer to it.

With the rapid development and complex challenges of chemical substances, the synthesis of new drugs is usually one of the most effective ways to increase yield.866775-18-0, name is Methyl 3-amino-6-bromo-5-(trifluoromethyl)picolinate, molecular formula is C8H6BrF3N2O2, molecular weight is 299.05, as common compound, the synthetic route is as follows.Recommanded Product: Methyl 3-amino-6-bromo-5-(trifluoromethyl)picolinate

3-Amino-6-bromo-5-trifluoromethyl-pyridine-2-carboxylic acid methyl ester (Intermediate A step 4) (2 g, 6.69 mmol) was suspended in toluene (8 ml), then p-toluenesulfonic acid (TsOH) (0.1 15 g, 0.669 mmol) and acetonylacetone (0.941 ml, 8.03 mmol) was added. The reaction mixture was heated at reflux for 2 h and allowed to cool to RT overnight. The resulting dark red/ black solution was concentrated under reduced pressure to remove toluene and the crude residue was diluted with EtOAc (200 ml), washed with NaHC03 (50 ml), dried (MgS04) and concentrated under reduced pressure to give a brown solid; LC-MS Rt = 5.58 min [M+H]+ 377/379 (Method 10minl_C_v002). 1 H NMR (400 MHz, DMSO-d6) ? 8.50 (1 H, s), 7.77 (2H, s), 5.83 (3H, s), 1.90 (6H, s); 19F NMR (400 MHz, DMSO-d6) ? -62.26 (CF3, s)

At the same time, in my other blogs, there are other synthetic methods of this type of compound,866775-18-0, Methyl 3-amino-6-bromo-5-(trifluoromethyl)picolinate, and friends who are interested can also refer to it.

Reference:
Patent; NOVARTIS AG; LEGRAND, Darren Mark; WO2013/38378; (2013); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem