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发明授权
CN105622521B 一种瑞舒伐他汀钙关键中间体的制备方法 有权

一种瑞舒伐他汀钙关键中间体的制备方法
摘要：
本发明公开了瑞舒伐他汀钙中间体即式I所示化合物的制备方法，其包括如下步骤：a)以对氟苯乙酮与异丁酸乙酯反应制备式IV化合物；b)所得化合物IV与甲基胍盐酸盐和氢氧化钾反应得到式III化合物；c)化合物III与三乙胺和甲磺酰氯反应制备式II化合物；d)式II与N,N‑二甲基甲酰胺和三氯氧磷反应得到式I化合物；其反应路线如下所示：本发明方法具有操作简单、所用原料价廉易得、反应条件温和、设备要求、生产成本低、易于规模化生产等优点，具有显著性工业应用价值。
摘要（英）：

The invention discloses a preparation method of a rosuvastatin calcium key intermediate, i.e. a compound as shown in a formula I. The preparation method comprises the following steps: a, carrying out a reaction between fluoroacetophenone and ethyl isobutyrate to prepare a compound as shown in a formula IV; b, carrying out a reaction between the obtained compound IV and methylguanidine hydrochloride as well as potassium hydroxide to obtain a compound as shown in a formula III; c, carrying out a reaction between the compound III and triethylamine as well as methanesulfonyl chloride to prepare a compound as shown in a formula II; d, carrying out a reaction between the compound as shown in the formula II and N,N-dimethylformamide as well as phosphorus oxychloride to obtain the compound as shown in the formula I. A reaction route of the preparation method is as shown in the following: (referring to the specification). The method disclosed by the invention has the advantages of being simple to operate, low in raw material price, high in availability of used raw materials, mild in reaction conditions, low in equipment requirements and production cost, easy for scale production and the like, and has significance industrial application value.

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