Development of a fully automated multichannel peptide synthesizer with integrated TFA cleavage capability.
Development of a fully automated multichannel peptide synthesizer with integrated TFA cleavage capability.
复制标题
开发具有集成 TFA 裂解功能的全自动多通道肽合成仪。
DOI：
--
复制
发表时间：
1993
期刊：
影响因子：
--
通讯作者：
J. Briand
中科院分区：
文献类型：
--
作者：
J. Neimark;J. Briand
一个全自动多通道肽合成仪已经建成，进行同步和快速组装的肽在20-200 μ mol规模。选择使用BOP或PyBOP原位活化氨基酸以得到优化的偶联化学。特殊设计的阀块，零死体积与原始电路相结合，允许分配预先溶解在DMF中的氨基酸衍生物和试剂。Boc或Fmoc化学可以在合成仪上进行调整。在Boc合成中，涉及纯TFA中的Boc基团脱保护，随后伴随中和和偶联步骤的非常快速的方案允许在每个通道上每小时添加三个氨基酸。在Fmoc化学中，我们将自动TFA切割系统集成到合成仪中，该系统允许肽直接在用于合成的反应器内从树脂上切割。研究了Fmoc氨基酸衍生物在DMF中的溶液中的稳定性，发现在合成的时间跨度期间分解不显著。通过对15-20肽段的常规合成，证明了仪器的良好性能。
A fully automated multichannel peptide synthesizer has been constructed which performs simultaneous and rapid assembly of peptides on a 20-200 mumol scale. In situ activation of amino acids using BOP or PyBOP was chosen to give an optimized coupling chemistry. Specially designed blocks of valves, with a zero dead volume combined with an original circuitry, permit the distribution of amino acids derivatives and reagents pre-dissolved in DMF. Either Boc or Fmoc chemistry can be adapted on the synthesizer. In Boc synthesis a very rapid protocol involving Boc group deprotection in neat TFA, followed by the concomitant steps of neutralization and coupling, allows the addition of three amino acids per hour on each channel. In Fmoc chemistry we have integrated into the synthesizer an automatic TFA cleavage system that allows the peptides to be cleaved from the resin directly within the reactors used for synthesis. The stability of the Fmoc amino acid derivatives in solution in DMF was investigated, and decomposition was found to be insignificant during the time-span of a synthesis. The satisfactory performance of the instrument was demonstrated by routine synthesis of 15-20 mer peptides.