| 盐酸硫胺(VB1)催化合成四氢咔唑类化合物 |
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| 引用本文： | 杨雅琴,葛松兰,马磊. 盐酸硫胺(VB1)催化合成四氢咔唑类化合物[J]. 医学教育探索, 2016, 0(4): 499-507 |
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| 作者姓名： | 杨雅琴 葛松兰 马磊 |
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| 作者单位： | 华东理工大学药学院, 上海市新药设计重点实验室, 上海 200237,华东理工大学药学院, 上海市新药设计重点实验室, 上海 200237,华东理工大学药学院, 上海市新药设计重点实验室, 上海 200237 |
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| 基金项目： | 上海自然科学基金（15ZR1408800）；上海浦江人才计划（15PJD0122015） |
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| 摘 要： | 1，2，3，4-四氢咔唑类衍生物广泛应用于医药领域。在盐酸硫胺（VB1）催化作用下，苯肼盐酸盐和环己酮在乙醇中反应，可以简便、高产率地得到四氢咔唑类化合物。将不同基团取代的环己酮和含有吸电子或供电子基团的苯肼用VB1进行底物扩展，大部分目标产物的产率在90%以上，证实在合成四氢咔唑的反应中，VB1是一种温和、高效、环保型的催化剂。对VB1进行回收再利用，催化效率没有明显降低。
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| 关 键 词： | 盐酸硫胺(VB1) 四氢咔唑 苯肼 环己酮 |
| 收稿时间： | 2015-11-27 |
Synthesis of Tetrahydrocarbazole Derivatives Using Thiamine Hydrochloride (VB1) as Efficient Catalyst |
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| YANG Ya-qin,GE Song-lan and MA Lei. Synthesis of Tetrahydrocarbazole Derivatives Using Thiamine Hydrochloride (VB1) as Efficient Catalyst[J]. Researches in Medical Education, 2016, 0(4): 499-507 |
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| Authors: | YANG Ya-qin GE Song-lan MA Lei |
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| Affiliation: | Shanghai Key Laboratory of New Drug Design, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China,Shanghai Key Laboratory of New Drug Design, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China and Shanghai Key Laboratory of New Drug Design, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China |
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| Abstract: | The tetrahydrocarbazole derivatives are widely used in pharmaceutical chemistry.A simple and highly efficient method was developed for the construction of tetrahydrocarbazole derivatives from phenylhydrazine hydrochloride and cyclohexanone in the presence of thiamine hydrochloride (VB1) in ethanol.This protocol relies on the use of various cyclohexanone and phenylhydrazine hydrochloride with electron-donating and electron-withdrawing groups to access tetrahydrocarbazole scaffolds with a wide scope.Most of the target products catalyzed by VB1 were obtained in good to excellent yields (>90%).VB1 acted as an efficient,mild and non-toxic catalyst in the reaction,and it could be reused without reducing the catalytic efficiency. |
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| Keywords: | thiamine hydrochloride (VB1) tetrahydrocarbazole phenylhydrazine cyclohexanone |
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