| 引用本文: | 苏信杰,张恺,周付刚,邢松松,杜玉民.抗肿瘤药物NSC-639829的合成[J].中国现代应用药学,2010,27(4):323-325. |
| .Synthesis of Antitumor Agent NSC-639829[J].Chin J Mod Appl Pharm(中国现代应用药学),2010,27(4):323-325. |
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| 摘要: |
| 目的 合成抗肿瘤药物NSC-639829。方法 以4-氨基-2-甲基苯酚为起始原料，经亲核取代、异氰酸酯化合成4-(5-溴-2-嘧啶氧基)-3-甲基苯基异氰酸酯，再与2-二甲氨基苯甲酰胺缩合得目标化合物NSC-639829。结果 目标化合物经质谱、核磁共振氢谱和元素分析确证其化学结构，经HPLC分析纯度达99.5%，总收率达40.2%。结论 此工艺路线原料易得，产品收率高，操作安全，适用于工业化生产。 |
| 关键词: NSC-639829 抗肿瘤药 合成 |
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| Synthesis of Antitumor Agent NSC-639829 |
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SU Xinjie ZHANG Kai ZHOU Fugang XING Songsong DU Yumin*
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| Abstract: |
| OBJECTIVE To synthesize antitumor agent NSC-639829. METHODS NSC-639829 was prepared from 4-amino-2-methylphenol via nucleophilic substitution, isocyanation, and condensation. RESULTS The total yield of NSC-639829 was amount to 40.2% with the purity of 99.5% by HPLC, and its structure was confirmed by MS, 1H-NMR, and elemental analysis. CONCLUSION The synthetic route for NSC-639829 was convenient for industrial manufacture. |
| Key words: NSC-639829 antitumor agent synthesis |
