| 张怀远,唐蓉萍.化学通报,2018,81(11):1048-1051. |
| 氟班色林的合成新方法 |
| A novel route of synthesis for Flibanserin |
| 投稿时间：2018-06-28 修订日期：2018-07-26 |
| DOI： |
| 中文关键词: 氟班色林 醋酸碘苯 苯并咪唑酮 合成 |
| 英文关键词:Flibanserin, Diacetoxyiodobenzene, Benzimidazolones, Synthesis |
| 基金项目:甘肃省高等学校科研项目（2018B-091和2017D-26）资助 |
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| 中文摘要: |
| 本文报道了药物氟班色林的合成新方法,是通过醋酸碘苯促进的苯甲醛、N-苯基羟胺和三甲基氰硅烷的一锅法反应首先构建氟班色林的重要骨架苯并咪唑酮结构,随后,与1,2-二溴乙烷反应得到中间体8,接着在浓盐酸中水解,得到中间体9,最后与哌嗪盐酸盐10反应,以29%的总收率得到氟班色林11,所有化合物都经过了1 H NMR、13 C NMR、HRMS表征,该方法具有原料价廉、易得,操作方便,副产物少,收率较高等特点。 |
| 英文摘要: |
| A novel and efficient synthesis of flibanserin was reported. One pot reaction of benzaldehyde, N-phenyl hydroxylamine and trimethylsilyl cyanide promoted by diacetoxyiodobenzene to construct benzimidazolones, which was the key skeleton structure of flibanserin, then, reaction with 1,2-Dibromoethane to generate compound 8, which was hydrolyzedSin concentrated hydrochloric acid toSproduce intermediate 9. At last, intermediate 9 was reacted with 10 to obtain flibanserin with a total yield of 29%. This method has the advantages of inexpensive raw material, easy operation, little byproduct and moderate yield. |
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