Preparation process of arotinolol hydrochloride intermediate

The invention discloses a preparation method of an arotinolol hydrochloride intermediate, and particularly, the preparation method comprises the following steps: firstly carrying out acylating chlorination reaction on 5-acetyl-thiophene-2-carboxylic acid to prepare intermediate acyl chloride, then c...

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Hauptverfasser: WANG YING, ZHANG TAO, LIU JIAN, CHEN HONG, QIAO ZHITAO, LIU TAO, LIN SONG
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention discloses a preparation method of an arotinolol hydrochloride intermediate, and particularly, the preparation method comprises the following steps: firstly carrying out acylating chlorination reaction on 5-acetyl-thiophene-2-carboxylic acid to prepare intermediate acyl chloride, then carrying out ammonolysis reaction to prepare an intermediate I, and finally reacting the intermediate I with a bromination reagent. The method has the beneficial effects that the reaction conditions of each step are mild, the reaction steps are short, the atom utilization rate is high, the operation is simple and controllable, the reaction yield is high, the product purity is high, a high-toxicity reagent is not used, environmental protection and labor protection are utilized, and the method is suitable for large-scale industrial production. 本发明公开了盐酸阿罗洛尔中间体的制备方法,具体而言,该制备方法包括将5-乙酰-噻吩-2-羧酸先经酰氯化反应制得中间态酰氯,再通过氨解反应制得中间体Ⅰ,中间体Ⅰ最后再与溴化试剂反应。本发明带来的有益效果有:各步骤反应条件温和、反应步骤短、原子利用率高、操作简单可控、反应收率高、产品纯度高、不使用高毒性试剂,利用环保和劳动保护,适合于大规模工业化生产。