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发明公开
CN102268029A 化合物（1S,2S,3R,5S）-蒎烷二醇-L-苯丙氨酸-L-亮氨酸硼酸酯的制备 有权

化合物（1S,2S,3R,5S）-蒎烷二醇-L-苯丙氨酸-L-亮氨酸硼酸酯的制备
摘要：
本发明公开了化合物（1S,2S,3R,5S）-蒎烷二醇-L-苯丙氨酸-L-亮氨酸硼酸酯（结构式1）的制备方法。由L-苯丙氨酸与三光气反应得到结构式8的化合物，化合物8与结构式7的化合物缩合得到单一构型的结构式1的化合物。化合物1与吡嗪甲酸缩合得到结构式10的化合物，化合物10经水解，得到抗癌药硼替佐米。本发明合成方法操作简便，收率高，原料易得，环境污染少。适合工业化生产。
摘要（英）：

The invention discloses a preparation method of a compound (1S, 2S, 3R, 5S)-pinanediol-L-phenylalanine-L-leucine boric acid ester (shown in the structural formula 1). The preparation method comprises the following steps that L-phenylalanine and triphosgene undergo a reaction to produce a compound shown in the structural formula 8; the compound shown in the structural formula 8 and a compound shown in the structural formula 7 undergo a condensation reaction to produce a compound which has a single configuration and is shown in the structural formula 1; the compound shown in the structural formula 1 and pyrazinecarboxylic acid undergo a condensation reaction to produce a compound shown in the formula 10; and the compound shown in the formula 10 is hydrolyzed to form bortezomib which is an anticancer drug. The preparation method has the advantages of simple operation, high yield, easy acquirement of raw materials, and low pollution on the environment. The preparation method is suitable for industrialized production.

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