Preparation method of brexpiprazole
The invention relates to a preparation method of brexpiprazole. The preparation method comprises the following steps: synthesizing a compound 1 by taking 4-substituted butyronitrile and 7-hydroxyquinoline-2-(1H) ketone as initial raw materials, reducing the compound 1 to obtain a compound 2, carryin...
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| Format: | Patent |
| Sprache: | chi ; eng |
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| Zusammenfassung: | The invention relates to a preparation method of brexpiprazole. The preparation method comprises the following steps: synthesizing a compound 1 by taking 4-substituted butyronitrile and 7-hydroxyquinoline-2-(1H) ketone as initial raw materials, reducing the compound 1 to obtain a compound 2, carrying out ring closing on the compound 2 and BOC-dichloro-ethylimine to obtain a compound 3, carrying out deprotection on the compound 3 to obtain a compound 4, and carrying out column chromatography on the compound 4 to obtain a compound 5. And reacting the compound 4 with 4-bromobenzothiophene to obtain the target product brexpiprazole. The method has the advantages of simple operation, easily controllable reaction, easily available raw materials, easily separated products, environmental friendliness and suitability for industrial production.
本发明涉及一种依匹哌唑的制备方法；所述制备方法包括以下步骤：以4-取代丁腈和7-羟基喹啉-2-(1H)酮为起始原料合成化合物1，再将化合物1还原得到化合物2，化合物2与BOC-双氯乙基亚胺关环得化合物3，化合物3经脱保护得化合物4，将化合物4和4-溴苯并噻吩反应得到目标产物依匹哌唑；本发明操作简单、反应易控、原料易得、产物容易分离、环境友好，适宜工业化 |
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