These common heterocyclic compound, 64628-73-5, name is 3-Chloro-4-(trifluoromethoxy)aniline, 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. COA of Formula: C7H5ClF3NO
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 , 0.14 mmol) and K3PO4 (446 mg, 2.1 mmol, 2.1 mL H2O), after stirring well, 3-chloro-4-trifluoromethoxyaniline (444 mg, 2.10 mmol) in toluene (4 mL) was added, protected by argon Then, the reaction was refluxed overnight, and a small amount of starting material remained. Cool to room temperature, concentrate, add EA (30mL) to dissolve the residue, 6N hydrochloric acid (10mL × 2), saturated brine (20mL × 3), water (20mL × 2), column chromatography (P / E = 20: 1 ~ 10: 1) to obtain 158 mg of a white solid with a yield of 54.3% and a melting point: 143-145 C.
The synthetic route of 3-Chloro-4-(trifluoromethoxy)aniline 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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