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经典酰胺偶联试剂的进一步应用:固相微波辅助酯化反应。

Further applications of classical amide coupling reagents: Microwave-assisted esterification on solid phase.

作者信息

Takayama Risa, Hayakawa Shun, Hinou Hiroshi, Albericio Fernando, Garcia-Martin Fayna

机构信息

Graduate School of Life Science, Hokkaido University, N21, W11, Kita-ku, Sapporo, 001-0021, Japan.

Faculty of Advanced Life Science, Hokkaido University, N21, W11, Kita-ku, Sapporo, 001-0021, Japan.

出版信息

J Pept Sci. 2018 Aug;24(8-9):e3111. doi: 10.1002/psc.3111. Epub 2018 Jul 16.

Abstract

Ester linkage (s) is a key chemical connector in organic chemistry, including natural products, peptides, and synthetic polymers. We herein describe a straightforward method for the efficient formation of ester linkage (s) on solid-phase. This method simply involves the use of amide coupling reagents under microwave irradiation. The robustness of this method relies on the use of classical solid-phase coupling reagents, heating by microwave irradiation, and a short time period, which results in high yields and the minimization of racemization.

摘要

酯键是有机化学中的关键化学连接键,包括天然产物、肽和合成聚合物。本文我们描述了一种在固相上高效形成酯键的直接方法。该方法仅涉及在微波辐射下使用酰胺偶联试剂。此方法的稳健性依赖于使用经典的固相偶联试剂、微波辐射加热以及较短的反应时间,这导致高产率和外消旋化的最小化。

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