| 硅胶催化的选择性去除N-Boc保护基 |
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| 引用本文： | 张敏杰,袁修华,马丽,赵剑英,高连勋. 硅胶催化的选择性去除N-Boc保护基[J]. 高等学校化学学报, 2007, 28(12): 2330-2332 |
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| 作者姓名： | 张敏杰 袁修华 马丽 赵剑英 高连勋 |
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| 作者单位： | 中国科学院长春应用化学研究所,高分子物理与化学国家重点实验室,长春,130022;中国科学院研究生院,北京,100049;中国科学院长春应用化学研究所,高分子物理与化学国家重点实验室,长春,130022 |
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| 摘 要： | 发现了在回流的甲苯中, 以硅胶为催化剂, 多种N-Boc保护的伯胺、仲胺、氨基酸的氨基都可以迅速脱除Boc. 该方法具有条件温和、操作简便、反应时间短和产率高等优点. 同时, 其它常用的保护基Cbz和Fmoc等在同样的条件下不受影响.
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| 关 键 词： | N-Boc脱保护 硅胶 选择性脱保护 |
| 文章编号： | 0251-0790（2007）12-2330-03 |
| 收稿时间： | 2007-06-12 |
| 修稿时间： | 2007-06-12 |
Selective Deprotection of N-Boc Catalyzed by Silica Gel |
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| ZHANG Min-Jie,YUAN Xiu-Hua,MA Li,ZHAO Jian-Ying,GAO Lian-Xun. Selective Deprotection of N-Boc Catalyzed by Silica Gel[J]. Chemical Research In Chinese Universities, 2007, 28(12): 2330-2332 |
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| Authors: | ZHANG Min-Jie YUAN Xiu-Hua MA Li ZHAO Jian-Ying GAO Lian-Xun |
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| Affiliation: | 1. State Key Laboratory of Polymer Physics and Chemistry, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun 130022, China; 2. Graduate School of Chinese Academy of Sciences, Beijing 100049, China |
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| Abstract: | As an important protective group of amines and amino acids, tert-butoxycarbonyl(Boc) group was extensively used in organic synthesis. Though many mild and selective reagents could be used, there is still a need for the development of a more simple and convenient method for deprotection. In this paper, a new method for the deprotection of N-Boc group with silica gel in refluxing toluene was reported. The reactions were mostly achieved in 5 h with high yields(75%—98%). N-Boc protected indoline and benzylamine, which are not deprotected with other mild method, could be deprotected with our method in good yields(89% and 95%, respectively). Additionally the deprotection of other carbamates such as Cbz, Fmoc and ethyl carbamate wasn’t observed under same conditions. |
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| Keywords: | N-Boc deprotection Silica gel Selective deprotection |
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