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OALib Journal期刊
ISSN: 2333-9721
费用：99美元
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[1-(5-氟戊基)-1h-吲哚-3-基](2-碘苯基)甲酮的合成
DOI: 10.3969/j.issn.1671-7627.2012.03.023, PP. 111-115
Keywords: 苯磺酰基保护,傅克酰基化,n-烷基化,酯水解,甲磺酰化,am-694的氟化
Abstract:
合成了具有较强的医学活性的[1-(5-氟戊基)-1h-吲哚-3-基](2-碘苯基)甲酮(am-694)。首先以吲哚为起始原料,苯磺酰氯保护吲哚的1-位,alcl3催化在吲哚3-位傅克酰基化的进行,避免了文献中通过格氏镁试剂(rmgx)对1-位的保护对无水、无氧的高要求,再将1-位保护脱掉,然后在1-位进行n-烷基化、酯基水解、甲磺酯化,最后用四正丁基氟化铵氟化。通过液相色谱(hplc)进行含量分析,且利用核磁(nmr)和质谱(ms)进行了表征,反应总收率高达41.8%。与以往路线相比,文中方法步骤简单,成本较低,收率很高。
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