Synthetic Route of 5211-02-9, These common heterocyclic compound, 5211-02-9, name is 3-Chloro-4-ethoxyaniline, 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.
4-Bromo-7-fluoro-1H-indole-2-carboxylic acid ethyl ester (200 mg, 0.7 mmol) was dissolved in toluene (16 mL), and Pd2 (dba) 3 (64 mg, 0.07 mmol) and Davephos (55 mg) were sequentially added. , 0.14 mmol) and K3PO4 (446 mg, 2.1 mmol, 2.1 mL of H2O), and after stirring well, 2- (4-amino-2-chlorophenoxy) ethyl-1-yl (394 mg, 2.10 mmol) of toluene ( 4mL) solution, under the protection of argon, refluxed for 20h. Cool to room temperature, concentrate, add EA (30mL) to dissolve the residue, 5N hydrochloric acid (20mL), saturated brine (20mL ¡Á 3), extract with water (20mL ¡Á 2), dry over anhydrous magnesium sulfate, and column chromatography (P / E = 5: 1 to 3: 1) 82 mg of a yellow solid was obtained with a yield of 29.9% and melting point: 191-192 C.
The synthetic route of 5211-02-9 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; Chinese Academy Of Medical Sciences Pharmaceutical Institute; Xu Boling; Chen Xiaoguang; Cui Guonan; Lai Fangfang; Zhou Jie; Ji Ming; Wang Xiaoyu; Du Tingting; Li Ling; Jin Jing; (144 pag.)CN110483366; (2019); A;,
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