用于生物共轭反应的TCO (反-环辛烯)试剂

TCO (反-环辛烯)作为一种能与四嗪进行应变促进的逆电子需求Diels-Alder环加成 (SPIEDAC)反应的化合物而被熟知。该反应作为生物共轭反应，广泛用于蛋白标记和成像^1-4)。4-TCO-NPC赤道异构体、4-TCO-NPC轴向异构体、2-TCO-NPC轴向异构体和2-TCO-NPC赤道异构体互相为位置及立体异构体，反应性各不相同。与四嗪的反应速率为4-TCO > 2-TCO、轴向 > 赤道向。另一方面，特别是有硫醇基存在的生物体内，稳定性为2-TCO > 4-TCO ⁵⁾。这些试剂容易在碳酸酯基的位置与伯胺发生反应，得到相应的氨基甲酸酯 。此外，当它与具有荧光官能团的四嗪反应时，SPIEDAC能使氨基甲酸酯具有荧光。

关键词

T4212

4-TCO-NPC赤道异构体

T4213

4-TCO-NPC轴向异构体

T4218

2-TCO-NPC轴向异构体

T4219

2-TCO-NPC赤道异构体

T3948

TCO-PEG3-马来酰亚胺

T3949

反-环辛烯-PEG4-NHS

T4126

N-(4E)-TCO-L-赖氨酸

文献

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