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发明公开
CN106986809A 一种5‑溴‑6‑氯‑3‑吲哚辛酯的合成方法 有权

一种5‑溴‑6‑氯‑3‑吲哚辛酯的合成方法
摘要：
本发明公开了一种5‑溴‑6‑氯‑3‑吲哚辛酯的合成方法，其特征在于，将4‑氯‑2‑氨基苯甲酸与N‑溴代丁二酰亚胺经过溴代反应得到5‑溴‑4‑氯‑2‑氨基苯甲酸，5‑溴‑4‑氯‑2‑氨基苯甲酸与氯乙酸钠经过亲核取代反应得到N‑(4‑溴‑5‑氯‑2‑羧基)苯基甘氨酸，N‑(4‑溴‑5‑氯‑2‑羧基)苯基甘氨酸再经环化脱羧反应得到1‑乙酰基‑5‑溴‑6‑氯‑3‑吲哚乙酯，1‑乙酰基‑5‑溴‑6‑氯‑3‑吲哚乙酯与辛酰氯选择性酯化反应得到5‑溴‑6‑氯‑3‑吲哚辛酯。本发明的5‑溴‑6‑氯‑3‑吲哚辛酯的合成方法，其高效、安全环保、反应总产率相对较高，因此可以用于5‑溴‑6‑氯‑3‑吲哚辛酯的大规模合成。
摘要（英）：

The invention discloses a 5-bromo-6-chloro-3-indolyl caprylate synthesis method, which is characterized in that 4-chloro-2-aminobenzoic acid and N-bromosuccinimide are subjected to a bromination reaction to obtain 5-bromo-4-chloro-2-aminobenzoic acid, 5-bromo-4-chloro-2-aminobenzoic acid and sodium chloroacetate are subjected to a nucleophilic substitution reaction to obtain N-(4-bromo-5-chloro-2-carboxy)phenylglycine, N-(4-bromo-5-chloro-2-carboxy)phenylglycine is subjected to a cyclization decarboxylation reaction to obtain 1-acetyl-5-bromo-6-chloro-3-indole ethyl ester, and 1-acetyl-5-bromo-6-chloro-3-indole ethyl ester and octanoyl chloride are subjected to a selective esterification reaction to obtain 5-bromo-6-chloro-3-indolyl caprylate. According to the present invention, the 5-bromo-6-chloro-3-indolyl caprylate synthesis method has advantages of high efficiency, safety, environmental protection and relatively high total reaction yield, and can be used for the large-scale synthesis of 5-bromo-6-chloro-3-indolyl caprylate.

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