Application of 876343-10-1 ,Some common heterocyclic compound, 876343-10-1, molecular formula is C6H3ClIN3, 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.
4-(4-(5-Fluoro-3-r4-(1-fluoro-cvclopropyl)-benzoylaminol-2-methyl-phenyl)-7H- Pyrrolor2 -dlpyrimidin-6-yl)-3,6-dihvdro-2H-pyridine-1-carboxylic acid dimethylamide(1 ) 4-(4-Chloro-7H-pyrrolor2,3-dlpyrimidin-6-yl)-3,6-dihvdro-2H-pyridine-1-carboxylic acid tert-butyl ester, Intermediate 1To a mixture of 4-chloro-6-iodo-7H-pyrrolo[2,3-d]pyrimidine (2.6 g, 9.30 mmol) and dichlorobis(triphenylphosphine)palladium (II) (0.52 g, 0.74 mmol) in 1-propanol (120 ml) and aqueous sodium carbonate solution (2M, 10.23 ml, 20.46 mmol), 4-(4, 4,5,5- tetramethyl-[1 ,2,3]dioxaborolan-2-yl)-3,6-dihydro-2H-pyridine-1-carboxylic acid tert-butyl ester (3.02 g, 9.77 mmol) was added. The mixture was heated to 100C for 18 hours. After cooling the brownish mixture was diluted with 200 ml water and extracted with DCM. The organic layer was washed with brine (2x) and dried over sodium sulfate, than filtered and evaporated. The residue was purified by flash chromatography on silica (cyclohexane/EtOAc 1 :1 ) to afford the compound Intermediate 1 as a beige solid.MS (ESI): 335 [M+H]+ , 1H-NMR (DMSO-d6): delta (ppm) 12.64 (br s, 1 H), 8.56 (s, 1 H), 6.59 (s, 2H), 4.08 (br s, 2H), 3.57 (m, 2H), 2.55 (m, 2H), 1.45 (s, 9H). (2) 4-Chloro-6-(1.2.3.6-tetrahvdro-pyridin-4-vn-7H-pyrrolor2.3-dlpyrimidine.
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,876343-10-1, its application will become more common.
Reference:
Patent; NOVARTIS AG; HENG, Richard; HOEGENAUER, Elizabeth, Kate; KOCH, Guido; PULZ, Robert, Alexander; VULPETTI, Anna; WAELCHLI, Rudolf; WO2013/8095; (2013); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia