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利伐沙班的合成工艺改进

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摘要 寻求工业化生产利伐沙班原料药的合成方法,以4-(4-氨基苯基)-3-吗茚酮和(S)-N-缩水甘油邻苯二甲酰亚胺为起始原料,经开环反应、与N,N-二羰基咪唑加成、在甲胺水溶液中胺解、最后与5-氯-2-酰氯噻吩加成得到利伐沙班粗品;后经冰乙酸一水重结晶、微粉化得到目标化合物。该路线操作简单,条件温和,生产成本低,适合工业化大规模生产。
出处 《现代盐化工》 2024年第1期4-5,共2页 Modern Salt and Chemical Industry
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