Electric Literature of 60811-21-4, These common heterocyclic compound, 60811-21-4, name is 4-Bromo-2-chloro-1-fluorobenzene, 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-Amino-6-bromo-1H-indole-2-carboxylic acid ethyl ester (200 mg, 0.71 mmol), Pd2 (dba) 3 (64 mg, 0.07 mmol), X-phos (82 mg, 0.14 mmol) and Cs2CO3 ( 684mg, 2.13mmol), 2-chloro-4-bromo-1-fluorobenzene (440mg, 2.13mmol) was added to a microwave tube, toluene (4mL) was added, argon protection, microwave reaction, reaction at 100 C for 4h, the raw materials disappeared. Cool to room temperature, add EA (30mL) to dissolve the residue, wash with saturated brine (20mL ¡Á 3), wash with water (20mL ¡Á 2), column chromatography (P / E = 30: 1 20: 1) to obtain 118mg of pale yellow solid. The yield is 44.55%. Melting point: 220-222 C.
The synthetic route of 60811-21-4 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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