Continuously updated synthesis method about 5-(Trifluoromethyl)pyrazin-2-amine

The synthetic route of 69816-38-2 has been constantly updated, and we look forward to future research findings.

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. 69816-38-2, name is 5-(Trifluoromethyl)pyrazin-2-amine belongs to pyrazines compound, it is a common compound, a new synthetic route is introduced below. Recommanded Product: 5-(Trifluoromethyl)pyrazin-2-amine

Heat a mixture of 5-chloro-2- (3-methylpyridin-2-yl)- [1, 8] naphthyridine (51 mg, 0.2 MMOL), 2-AMINO-5-TRIFLUOROMETHYLPYRAZINE (42.0 mg, 0. 25 MMOL), xantphos (11.6 mg, 0.02 mmol), Pd2 (dba) 3 (18.3 mg, 0.02 mmol) and Cs2CO3 (130 mg, 0.4 mmol) in dioxane (2.0 mL) at 100C for 20 HOURS. COOL the mixture, concentrate under vacuum, dilute with EtOAc/ water (5.0 mL each), filter through celite, wash celite with EtOAc (2 x 5 mL) and dry the combined organic layers with MGS04. Filter the dried extract and concentrate under vacuum to afford the crude product. Purify by preparative TLC using 2% MEOH/ETOAC as eluent to afford the title compound as a yellow SOLID. H NMR (400 MHZ, DMSO-D6) 8 10.6 (s, 1H), 9.04 (d, 1H, J=2.1 Hz), 9.0 (s, LH), 8.77 (s, 2H), 8.59 (d, 1H, J=1.6 Hz), 8.4 (s, 1H), 8.20 (d, 1H, J=2. 2 Hz), 7. 81 (d, IH, J=L. 9 Hz), 7.42 (dd, 1H), 2.65 (s, 3H). MS = 383. 11 (M+H).

The synthetic route of 69816-38-2 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; NEUROGEN CORPORATION; WO2005/7652; (2005); A2;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Simple exploration of 69816-38-2

Statistics shows that 5-(Trifluoromethyl)pyrazin-2-amine is playing an increasingly important role. we look forward to future research findings about 69816-38-2.

Application of 69816-38-2, These common heterocyclic compound, 69816-38-2, name is 5-(Trifluoromethyl)pyrazin-2-amine, 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.

Step 2: 3-{4-Trifluoromethyl-2-[3-(5-tri-fluoromethyl-pyrazin-2-yl)-ureido]-phenoxymethyl}-piper-idine-1-carboxylic acid tert-butyl ester. 3-[2-(4-Nitro-phenoxycarbonylamino) -4-trifluoromethyl-phenoxymethyl] -piperidine-1-carboxylic acid tert-butyl ester (217 mg, 0.4 mmol) and 5-trifluoromethyl-pyrazin-2-ylamine (66 mg, 0.4 mmol) (prepared according to the method of U.S. 4,293,552) were mixed as solids in a 5 mL reaction vial, diluted with 400 uL NMP, capped and stirred as a darkyellow solution that then was immersed in an oil bath at 85C and stirred for six hours. The reaction mixture was cooled to room temperature and stirred overnight. NMP then was removed by Kugelrohr distillation at 0.5 mm and 80C. The brown residue was diluted to 30 mL with CH2C12 then washed 3 x 30 mL with 1M Na2C03 to remove p-nitro-phenol. The organics were dried (MgS04) , filtered, and concentrated to a crude solid that was triturated with EtOAc and filtered to give the desired product as a white solid.

Statistics shows that 5-(Trifluoromethyl)pyrazin-2-amine is playing an increasingly important role. we look forward to future research findings about 69816-38-2.

Reference:
Patent; ICOS CORPORATION; WO2006/21002; (2006); A2;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem