噻唑并[4,3-b]吡喃通过 DNA 上的[4 + 2]环加成反应构建。
Construction of Thiazole-Fused Dihydropyrans via Formal [4 + 2] Cycloaddition Reaction on DNA.
机构信息
Department of Therapeutic Discovery, 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.
出版信息
Org Lett. 2020 Apr 17;22(8):3239-3244. doi: 10.1021/acs.orglett.0c01016. Epub 2020 Apr 3.
An efficient and facile formal [4 + 2] cycloaddition reaction was developed to synthesize diverse thiazole-fused dihydropyrans (TFDP) on DNA. Mild reaction conditions, broad substrate scope, and compatibility with subsequent enzymatic ligation demonstrated the utility of this methodology in DNA-encoded library synthesis.
开发了一种高效且简便的形式[4 + 2]环加成反应，用于在 DNA 上合成各种噻唑并二氢吡喃（TFDP）。温和的反应条件、广泛的底物范围以及与后续酶连接的兼容性证明了该方法在 DNA 编码文库合成中的实用性。
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