具有 C5 位反应性基团的尿嘧啶核苷：5-(1-卤代-2-亚磺酰基乙烯基)尿苷类似物。
Uracil Nucleosides with Reactive Group at C5 Position: 5-(1-Halo-2-sulfonylvinyl)uridine Analogues.
机构信息
Department of Chemistry and Biochemistry, Florida International University , Miami, Florida 33199, United States.
出版信息
Org Lett. 2016 Mar 18;18(6):1418-21. doi: 10.1021/acs.orglett.6b00346. Epub 2016 Mar 2.
PMID:26933954
Abstract
The transition-metal-catalyzed or radical-mediated halosulfonylation of 5-ethynyluridine provided (E)-(1-halo-2-tosylvinyl)uridines. These (β-halo)vinyl sulfones undergo efficient stereoselective addition-elimination with amines or thiols to provide Z-β-aminovinyl or E-β-thiovinyl sulfones tethered to the C5 position of the uracil ring.
摘要
过渡金属催化或自由基介导的 5-乙炔基尿苷的卤磺酰化反应提供了（E）-（1-卤代-2-对甲苯磺酰基乙烯基）尿嘧啶。这些（β-卤代）乙烯基砜与胺或硫醇发生高效的立体选择性加成消除反应，在尿嘧啶环的 C5 位上提供了 Z-β-氨甲酰基乙烯基或 E-β-硫代乙烯基砜。
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