JQ1合成工艺的改进
Improvement of the synthetic technology of JQ1
作者：肖音;高源;顾宇虹;汤志强;
Author：
收稿日期： 年卷（期）页码：2018,33(03):-239-241
期刊名称：华西药学杂志
Journal Name：WEST CHINA JOURNAL OF PHARMACEUTICAL SCIENCES
关键字：JQ1;抗肿瘤药物;工艺改进;合成;4-氯苯甲酰基乙腈
Key words：
基金项目：
中文摘要
目的改进JQ1的合成工艺。方法以4-氯苯甲酰基乙腈为原料,与丁酮和硫在碱性条件下环合得到中间体Ⅴ[(2-氨基-4,5-二甲基噻吩-3-基)(4-氯苯基)甲酮];中间体Ⅴ再与9-芴甲氧羰基-天冬氨酸-β-叔丁基酯成酰胺后,脱保护得到中间体Ⅲ[(S)-3-氨基4-((3-(4-氯苯甲酰基)-4,5-二甲基噻吩-2-基)氨基)-4-氧丁酸叔丁酯],后者经环合、构建三唑环,得到目标化合物JQ1。结果与结论通过1HNMR、13CNMR、MS及IR对目标产物进行了结构确证,HPLC检测其纯度达100%;以原料4-氯苯甲酰基乙腈计算,产物的总收率为21.2%。
参考文献
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