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用于全保护肽制备的伪 Wang 柄。通过片段缩合合成利拉鲁肽。

Pseudo-Wang Handle for the Preparation of Fully Protected Peptides. Synthesis of Liraglutide by Fragment Condensation.

机构信息

CIBER-BBN, Networking Centre on Bioengineering, Biomaterials and Nanomedicine , University of Barcelona , 08028 Barcelona , Spain.

Institute of Advanced Chemistry of Catalonia (IQAC-CSIC) , Spanish National Research Council (CSIC) , 08034 Barcelona , Spain.

出版信息

Org Lett. 2019 Apr 5;21(7):2459-2463. doi: 10.1021/acs.orglett.9b00813. Epub 2019 Mar 14.

Abstract

A handle for the protection of the C-terminus of peptides after cleaving with low concentration of trifluoroacetic acid (2-4%) is reported. The handle prevents polymerization reactions in the convergent condensation of peptidic fragments. Moreover, it is traceless, being removed during the final deprotection step of the peptide synthesis. This cheap and convenient handle is easily attached to the solid support, causing no disturbance to peptide elongation and thus proving to be useful in the convergent synthesis of long peptides.

摘要

报道了一种在低浓度三氟乙酸(2-4%)裂解后保护肽 C 末端的方法。该手柄可防止肽片段缩合时的聚合反应。此外,它是无痕的,在肽合成的最后脱保护步骤中被去除。这种廉价且方便的手柄很容易连接到固体载体上,不会干扰肽的延伸,因此在长肽的缩合合成中非常有用。

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