Application of 762240-92-6, These common heterocyclic compound, 762240-92-6, name is 3-(Trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine hydrochloride, 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.
Azetidinone IIa’ (0.5 g, 2.32 mmol, ee 99.5 %), 3-(trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4] triazolo[4,3-a] pyrazine hydrochloride (III’, 1.06 g, 4.65 mmol), Et3N (0.28 g, 4.65 mmol) and 2-ethylhexanoic acid (0.17 g, 1.16 mmol) were suspended in THF (10 mL). The resulting suspension was stirred at 75C for 72 h. After cooling the mixture to 0C, compound 2 was filtered off and the solvent was removed in vacuo. To the remaining oil was added water (10 mL) and the product was extracted with dichloromethane (3 x10 mL). The organic phases were combined, dried over magnesium sulfate and concentrated in vacuo to give 0.90 g of sitagliptin (IV”) (95%, ee 99.5 %) as dark yellow oil.
Statistics shows that 3-(Trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine hydrochloride is playing an increasingly important role. we look forward to future research findings about 762240-92-6.
Reference:
Patent; LEK Pharmaceuticals d.d.; The designation of the inventor has not yet been filed; EP2674432; (2013); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem