The Petasis three-component reaction gives rise to diverse substituted α-aryl glycines from readily available amines, boronic acids and glyoxalic acid. Thus, this reaction is highly attractive for DNA-encoded small molecule screening library synthesis. The Petasis reaction is for instance promoted by a potentially DNA damaging copper(I)/bipyridine reagent system in dry organic solvents. We found that solid phase-coupled DNA strands tolerated this reagent system at elevated temperature allowing for synthesis of diverse substituted DNA-tagged α-aryl glycines from DNA-conjugated secondary amines.

中文翻译：

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铜/联吡啶促进的Petasis反应翻译成固相偶联的DNA以进行编码的文库合成

Petasis三组分反应从容易获得的胺，硼酸和乙二醛酸中产生各种取代的α-芳基甘氨酸。因此，该反应对于DNA编码的小分子筛选文库合成非常有吸引力。例如，在干燥的有机溶剂中，潜在破坏DNA的铜（I）/联吡啶试剂系统可促进Petasis反应。我们发现固相偶联的DNA链在高温下耐受该试剂系统，从而可以从DNA偶联的仲胺合成各种取代的DNA标记的α-芳基甘氨酸。