Analyzing the synthesis route of 4949-13-7

Statistics shows that 2-Fluoropyrazine is playing an increasingly important role. we look forward to future research findings about 4949-13-7.

Reference of 4949-13-7, These common heterocyclic compound, 4949-13-7, name is 2-Fluoropyrazine, 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.

2-fluoropiperidine4a (6 mL, 74.20 mmol) and cyclopropyl nitrile (5.74 mL, 77.9 mmol) were dissolved in dry toluene (60 mL).Nitrogen protection, 0 C, Sodium bis(trimethylsilyl)amide (39 mL, 78 mmol) was slowly added, and the reaction was naturally stirred at room temperature for 4 hours. The reaction was quenched by dropwise addition of saturated aqueous ammonium chloride (100 mL), and extracted with ethyl acetate (300 mL×2). The combined organic phase was washed with saturated sodium chloride solution (200 mL×2) Sodium drying, suction filtrationThe residue was purified by silica gel column chromatography (EtOAc/EtOAc (EtOAc)A pale yellow solid 4b (1.34 g, yield 12%) was obtained.

Statistics shows that 2-Fluoropyrazine is playing an increasingly important role. we look forward to future research findings about 4949-13-7.

Reference:
Patent; Guangdong Dongyangguang Pharmaceutical Co., Ltd.; Li Jianhao; Gu Zheng; Tang Wanjun; Kang Panpan; (43 pag.)CN109721555; (2019); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem