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

Pseudo-Wang Handle for the Preparation of Fully Protected Peptides. Synthesis of Liraglutide by Fragment Condensation
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DOI:
10.1021/acs.orglett.9b00813
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发表时间:
2019-04-05
期刊:
影响因子:
5.2
通讯作者:
Albericio, Fernando
Albericio, Fernando
中科院分区:
化学1区
文献类型:
--
作者:
Carbajo, Daniel;Fransen, Peter;Albericio, Fernando

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报道了一种用低浓度三氟乙酸(2-4%)切割后保护肽C-末端的手柄。柄防止肽片段的会聚缩合中的聚合反应。此外,它是无痕的,在肽合成的最终脱保护步骤期间被去除。这种便宜和方便的手柄容易连接到固体支持物上,不会干扰肽的延伸,因此证明在长肽的会聚合成中是有用的。
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.