Reference of 486460-21-3, In the next few decades, the world population will flourish. As the population grows rapidly and people all over the world use more and more resources, all industries must consider their environmental impact. 486460-21-3, name is 3-(Trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine belongs to Pyrazines compound, it is a common compound, a new synthetic route is introduced below.
DIPEA (0.307 mL, 1.759 mmol) was added to a mixture of 3-(trifluoromethyl)-5,6,7,8- tetrahydro-[ 1 ,2,4jtriazolo[4,3-ajpyrazine (127 mg, 0.660 mmol), cis-1 -(6-chloro-3- cyanoquinolin-4-yl)-2-methylpiperidine-4-carboxylic acid (145 mg, 0.440 mmol), and HATU(334 mg, 0.879 mmol) in DMF (4 mL) and stirred at 18 C for 3 h. The reaction was quenchedwith water (30 mL) and extracted with EtOAc (30 mL x 4), the combined organic phases were washed with brine (30 mL), dried over Na2SO4, filtered. The filtrates were concentrated and purified by p-HPLC to give cis-6-chloro-4-(2-methyl-4-(3-(trifluoromethyl)-5 ,6,7, 8-tetrahydro- [1 ,2,4jtriazolo [4,3-ajpyrazine-7-carbonyl)piperidin- 1 -yl)quinoline-3 -carbonitrile. MS: 504 (M + 1). The product was resolved by SFC (Column: Chiralpak AD-3 Mobile phase: A: CO2 B: methanol (0.05% DEA) Gradient: from 5% to 40% of B SFC separation gave peak 1(70mg, 0.135 mmol) MS: 504 (M + 1); and peak 2 (R,R or S,S) MS: 504 (M +1)
The synthetic route of 3-(Trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine has been constantly updated, and we look forward to future research findings.
Reference:
Patent; MERCK SHARP & DOHME CORP.; CUMMING, Jared, N.; DYKSTRA, Kevin, D.; HRUZA, Alan; LI, Derun; LIU, Hong; TANG, Haiqun; TAOKA, Brandon, M.; VERRAS, Andreas; WALSH, Shawn, P.; WU, Wen-Lian; (170 pag.)WO2018/34918; (2018); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem