Peptide synthesis. Part 5. Solid-phase synthesis of [15-leucine]little gastrin

Peptide synthesis. Part 5. Solid-phase synthesis of [15-leucine]little gastrin
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肽合成。

DOI:
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发表时间:
1983
期刊:
影响因子:
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通讯作者:
B. Williams
B. Williams
中科院分区:
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文献类型:
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作者:
E. Brown;R. Sheppard;B. Williams

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以[15-亮氨酸]小分子胃泌素为例,介绍了一种固相合成胃泌素肽的方法。该方法利用了极性聚酰胺树脂载体和逐步添加的荧甲氧基甲氧基氨基酸衍生物。最大限度地减少了酸性试剂的处理,消除了色氨酸侧链保护的需要,并消除了多个谷氨基残基上的酸催化副反应。末端焦谷氨基残基的形成是通过谷氨酰基中间体实现的。
A procedure is described for the solid-phase synthesis of gastrin peptides exemplified by [15-leucine]little gastrin. The method makes use of a polar polyamide resin support and stepwise addition of fluorenylmethoxycarbonylamino-acid derivatives. Treatment with acidic reagents is minimised, obviating the need for side-chain protection of tryptophan and eliminating acid-catalysed side reactions at the multiple glutamyl residues. Formation of the terminal pyroglutamyl residue was achieved through a glutaminyl intermediate.