Department of Discovery Modalities , Amgen Asia R&D Center, Amgen Research , 4560 Jinke Road , Pudong, Shanghai 201210 , P. R. China.
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica , Chinese Academy of Science , 501 Haike Road, Zhang Jiang Hi-Tech Park , Pudong, Shanghai 201203 , P. R. China.
Org Lett. 2018 Nov 16;20(22):7186-7191. doi: 10.1021/acs.orglett.8b03114. Epub 2018 Oct 26.
The synthesis of pyridazines on DNA has been developed on the basis of inverse-electron-demand Diels-Alder (IEDDA) reactions of 1,2,4,5-tetrazines. The broad substrate scope is explored. Functionalized pyridazine products are selected for subsequent DNA-compatible Suzuki-Miyaura coupling, acylation, and SAr substitution reactions, demonstrating the feasibility and versatility of IEDDA reactions for DNA-encoded library synthesis.
基于 1,2,4,5-四嗪的逆电子需求 Diels-Alder (IEDDA) 反应，开发了在 DNA 上合成哒嗪的方法。探索了广泛的底物范围。选择功能化的哒嗪产物进行后续的 DNA 相容的 Suzuki-Miyaura 偶联、酰化和 SAr 取代反应，证明了 IEDDA 反应在 DNA 编码库合成中的可行性和多功能性。
