These common heterocyclic compound, 15205-15-9, name is 2-Chloro-6-fluorobenzylamine, 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. Safety of 2-Chloro-6-fluorobenzylamine
General procedure: The pyrrole-3-carbaldehyde 3a-d (0.5 mmol) and a series of primary amines (0.6 mmol) were dissolved in dichloromethane (8 mL), and the resulting mixture was stirred for 30 min. The reaction was cooled at 0 C, and then NaBH(AcO)3 (1.25 mmol) and AcOH (0.5 mmol) were carefully added. The resulting mixture was stirred at room temperature for 16 h. The reaction was quenched with NaOH (1.0 M, 20 mL) and the product was extracted with ethyl acetate (3×25 mL). The organic extract was dried over anhydrous Na2SO4, filtered and evaporated in vacuo. The crude product was purified on the silica gel to afford 4a-b, 5a-c, 6a-r as yellow oil. Samples were dissolved in dichloromethane, and hydrogen chloride in diethyl ether solution (2.0M, 0.5mL) was added dropwise. The solvent was removed under reduced pressure to obtain pure solids as nuclear magnetic samples.
The synthetic route of 2-Chloro-6-fluorobenzylamine has been constantly updated, and we look forward to future research findings.
Reference:
Article; Wang, Ting; Tang, Yunxiang; Yang, Yang; An, Qi; Sang, Zitai; Yang, Tao; Liu, Pingxian; Zhang, Tianyu; Deng, Yong; Luo, Youfu; Bioorganic and Medicinal Chemistry Letters; vol. 28; 11; (2018); p. 2084 – 2090;,
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