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摘要
提出了一种新型绿色多肽合成方法,并成功将该方法应用于水蛭素的二十肽类似物Bivalirudin的合成。以苄氧羰基(Cbz)为氨基保护基,利用钯炭装填柱快速脱去Cbz保护,偶联反应及其后处理在微通道反应器内完成,实现了偶联-后处理-脱保护全体系的连续化。结果表明,相比于传统多肽合成方法,该方法原子经济性高、环境污染小,有望在多肽合成产业中得到更加广泛地应用。
Abstract
A novel green peptide synthesis method is proposed, and successfully applied to the synthesis of Bivalirudin, an icosapeptide analogue of hirudin.Benzyloxycarbonyl (Cbz) is used as a protecting group for amino, while the protection is rapidly removed in a column packed with Pd/C catalyst.The coupling reaction and its post-treatment are finished in a microchannel reactor via continuous flowing process, which achieves the continuity of the coupling-posttreatment-deprotection system.It is verified that this method shows a higher atom economy and fewer environment pollution than traditional peptide synthesis methods, it is expected to be more widely used in the peptide synthesis industry.
关键词
连续流动化学
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多肽合成
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比伐芦定
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微通道反应器
Key words
continuous flow chemistry
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peptide synthesis
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Bivalirudin
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microchannel reactor
Author summay
王振炜(1997-),男,硕士生,研究方向为多肽合成,15684736925@163.com
基于连续流动化学的Bivalirudin绿色合成方法的研究[J].
现代化工, 2023, 43(11): 140-144,149 DOI:10.16606/j.cnki.issn0253-4320.2023.11.027