Extracurricular laboratory: Synthetic route of 54608-52-5

The synthetic route of 54608-52-5 has been constantly updated, and we look forward to future research findings.

Application of 54608-52-5, These common heterocyclic compound, 54608-52-5, name is 2-Hydrazinopyrazine, 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.

Synthesis of 4-bromo-A, -(pyrazin-2-yl)benzohydrazide (15): 4-Bromohcnzoic acid (0.5 g, 2.4 mmol) was dissolved in dichloromethane (20 mL) and cooled to 0 C. 2- Hydrazinylpyrazine (0.32 g, 2.9 mmol), EDCI (0.55 g, 2.9 mmol), HOBt (0.39 g, 2.9 mmol) and DIPEA (0.96 g, 7.4 mmol) were added at 0 C. The reaction mixture was allowed to warm to room temperature and stirred for 4 h. The reaction mixture was transferred into water (100 mL) and extracted with CH2C12 (3 x 25 mL). The combined organic layers were washed with brine, dried over anhydrous Na2S04 and concentrated under reduced pressure to give crude product, which was purified by silica gel chromatography (0-5% MeOH in CH2C12) to obtain 4-bromo-N’-(pyrazin-2-yl)benzohydrazide (15). (Yield: 0.15 g, 20%). LCMS: m/z 295. 18 [M+2], = 1.8 min.

The synthetic route of 54608-52-5 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; KARYOPHARM THERAPEUTICS INC.; BALOGLU, Erkan; SHACHAM, Sharon; SENAPEDIS, William; MCCAULEY, Dilara; LANDESMAN, Yosef; GOLAN, Gali; KALID, Ori; SHECHTER, Sharon; WO2015/3166; (2015); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem