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使用热辐射和可控微波辐射的快速固相肽合成

Rapid solid-phase peptide synthesis using thermal and controlled microwave irradiation.

作者信息

Bacsa Bernadett, Desai Bimbisar, Dibó Gábor, Kappe C Oliver

机构信息

Institute of Chemistry, Eötvös Loránd University, H-1518 Budapest 112, Hungary.

出版信息

J Pept Sci. 2006 Oct;12(10):633-8. doi: 10.1002/psc.771.

Abstract

A rapid and efficient microwave-assisted solid-phase synthesis method is described for the preparation of the nonapeptide WDTVRISFK, using conventional Fmoc/Bu(t) orthogonal protection strategy. The synthesis protocol is based on the use of cycles of pulsed microwave irradiation with intermittent cooling of the reaction during the removal of the Fmoc protecting group and during the coupling. The desired nonapeptide was obtained in highest yield and purity by employing MicroKan technology. The chemical reactions were carried out in a single-mode microwave reactor, equipped with a fiber-optic probe to monitor the reaction temperature continuously.

摘要

描述了一种快速有效的微波辅助固相合成方法,用于制备九肽WDTVRISFK,采用传统的Fmoc/Bu(t)正交保护策略。合成方案基于在去除Fmoc保护基团和偶联过程中使用脉冲微波辐照循环并间歇冷却反应。通过采用MicroKan技术,以最高产率和纯度获得了所需的九肽。化学反应在配备有光纤探头以连续监测反应温度的单模微波反应器中进行。

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