Application of 3279-95-6 ,Some common heterocyclic compound, 3279-95-6, molecular formula is C2H7NO2, 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.
A four-neck 12 L round bottomed flask equipped with a mechanical stirrer, a thermocouple, an addition funnel, and a nitrogen inlet/outlet was charged with 7-(4-Bromo-2- fluoro-phenylamino)-6-methyl-5-oxo- 1,2,3, 5-tetrahydro-indolizine-8-carboxylic acid (I-2c: 400 g, 1.05 mol), PyBOP (707 g, 1.36 mol) and tetrahydrofuran (5.2 L) under nitrogen. The suspension was stirred at 17C for 5 minutes and triethylamine ( 176 mL, 1.26 mol) was added to the mixture. The mixture was stirred at 20C for 30 minutes and a solution was obtained. 2-(Aminooxy)ethanol (105 g, 1.36 mol) was added to the mixture. The resulting mixture was stirred at 20C for 30 minutes and then seeded with Compound 1 (0.3 g). The mixture was stirred at 20 C for 2 hours and filtered. The filter cake was rinsed with tetrahydrofuran (0.8 L) and dried in a vacuum oven at 40C/5 torr for 1 hour to yieldCompound 1 (370 g, 80%) as a white solid. [M+H] calculated for Ci8H1979BrFN304, 440; found, 440.1H NMR (DMSO-D6): delta 11.20 (s, 1H), 7.65 (s, 1H), 7.48 (d, 1H), 7.18 (d, 1H), 6.5 (t, 1H), 4.0 (t, 2H), 3.7 (t, 2H), 3.5 (s, 3H), 3.2 (t, 2H), 2. 14 (quin, 2H), 1.72 ( s, 3H).
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,3279-95-6, its application will become more common.
Reference:
Patent; NOVARTIS AG; WAYKOLE, Liladhar Murlidhar; KARPINSKI, Piotr H.; WO2011/67348; (2011); A2;,
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