Some common heterocyclic compound, 762240-92-6, name is 3-(Trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine hydrochloride, molecular formula is C6H8ClF3N4, 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. Safety of 3-(Trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine hydrochloride
The title compound was prepared using the method described in WO 2008/040974.A mixture of 3-nitropropionic acid (20.0 g, 0.168 mol), 3-(trifluoromethyl)-5,6,7,8-tetrahydro-[1 ,2,4]triazolo[4,3- a]pyrazine hydrochloride (48.0 g, 0.21 mol) in acetonitrile (400 mL) is cooled to 0 C and 4-methylmorpholine (16.9 g, 0.168 mol) is added, followed by N-(3-dimethylaminopropyl)-N’-ethylcarbodiimide hydrochloride (EDC) (48.4 g, 0.25 mol) after 5 min. The resulting mixture is stirred at room temperature for 20 hours. The resulting mixture is concentrated to about 2/3 of its volume and ethyl acetate is added (750 mL). The resulting mixture is washed twice with water (200 + 100 mL), sat. aq. sodium hydrogencarbonate (200 mL), brine (200 mL) and dried with sodium sulfate. The resulting clear solution is concentrated under reduced volume and MTBE is added (100 mL). The precipitated white solid is filtered off, washed with MTBE (200 mL) and dried under reduced pressure to yield 38.8 g (79 % yield) of NTPT as white powder.
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 762240-92-6, its application will become more common.
Reference:
Patent; LEK PHARMACEUTICALS D.D.; STERK, Damjan; USTAR, Matjaz; ZLICAR, Marko; WO2011/151443; (2011); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem