Photolabile Linkers for Solid-Phase Synthesis,ACS Combinatorial Science

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Photolabile Linkers for Solid-Phase Synthesis
ACS Combinatorial Science Pub Date : 2018-06-04 00:00:00 , DOI: 10.1021/acscombsci.8b00028
Remi J. T. Mikkelsen ₁ , Katja E. Grier ₁ , Kim T. Mortensen ₁ , Thomas E. Nielsen _{1,

2,

3} , Katrine Qvortrup ₁

Affiliation

Photolabile linkers are the subjects of intense research because they allow the release of the target molecule simply by irradiation. Photochemical release of synthesis products is often facilitated without additional reagents under mild reaction conditions, which may even be environmentally friendly and appealing in the context of greener chemistry. The mild conditions also allow for applications of released material in subsequent biological screening experiments, where contamination with cleavage reagents would be detrimental. This Review pays attention to the increasing number of photolabile linkers developed for solid-phase synthesis and release and covers: (i) o-nitrobenzyloxy linkers, (ii) o-nitrobenzylamino linkers, (iii) α-substituted o-nitrobenzyl linkers, (iv) o-nitroveratryl linkers, (v) phenacyl linkers, (vi) p-alkoxyphenacyl linkers, (vii) benzoin linkers, (viii) pivaloyl linkers, and (ix) other photolabile linkers.

中文翻译：

用于固相合成的光不稳定连接基

光不稳定性连接子是深入研究的主题，因为它们允许仅通过辐射来释放靶分子。在温和的反应条件下，通常无需合成试剂即可促进合成产物的光化学释放，这在环保化学的情况下甚至可能对环境友好且具有吸引力。温和的条件还允许释放的物质用于随后的生物筛选实验，在这种情况下，裂解试剂的污染将是有害的。该评论关注为固相合成和释放而开发的光不稳定连接体的数量不断增加，涉及以下方面：（i）邻硝基苄氧基连接基，（ii）邻硝基苄氨基连接基，（iii）α-取代的邻位-硝基苄基连接基，（iv）邻硝基veratryl连接基，（v）苯甲酰基连接基，（vi）对-烷氧基苯酰基连接基，（vii）安息香连接基，（viii）新戊酰基连接基和（ix）其他对光不稳定的连接基。

更新日期：2018-06-04

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