氯法拉滨是临床上唯一可以特异性地治疗儿童白血病的药物[1]。但是现有合成方法存在路线长、收率低和α/β异构体难以分离等问题[2,3]。本文以廉价且商品化的2-氯腺苷和自制苯炔基核糖为原料,通过Vorbrüggen糖苷化方法,利用金催化剂在温和条件下选择性地脱除2位的保护基。然后,以商品化的氟代试剂二乙胺基三氟化硫(DAST)进行2位羟基的氟代反应[4],再使用NH3/MeoH饱和溶液脱除乙酰基可得
The 3-cyclopropylideneprop-2-en-1-ones,which contain the highly strained cyclopropyl ring and carbonyl group adjacent to the two ends of cumulated double bonds,are a class of thermally stable,yet acti
The catalytic asymmetric synthesis of enantioenriched indole derivatives has aroused great concern in the community of chemistry because chiral indole frameworks constitute the core structures of many
Oxygen and sulfur-containing heterocyclic frameworks exist in lots of natural products and biologically important compounds.So,the construction of such scaffolds has absorbed much attention from the c
Among oxygen-containing heterocyclic frameworks,chiral 3,4-dihydroisocoumarin scaffold constitutes the core structures of many biologically important natural or unnatural compounds.On the other hand,s
Tetronic acid derivatives belong to one of the most important classes of natural products and pharmaceuticals,so the synthesis and biological evaluation of tetronic acid derivatives have absorbed grea
The spirocyclic oxindole-cylopentene skeletons featured in a large number of nature products have potential biological activity.Therefore,various approaches such as phosphine catalysis,and metal-media
3,4-Dihydrocoumarin derivatives have demonstrated promising biological activities as natural products and pharmaceuticals.Therefore,much attention has been paid on the development of efficient approac
手性吲哚衍生物作为一种杂环化合物,广泛存在于许多天然产物和药物活性分子中.所以,高效构建这种骨架,得到高对映选择性的产物已成为化学工作者的一个重要课题1.3-吲哚醇可以在酸性条件下质子化,变成烯丙基正离子或烯亚胺正离子,经常被人们在不对称环加成反应中使用2.而基于C3位不带取代基的2-吲哚醇的研究却很少3.该底物在布朗斯特酸的存在下,可以失去一分子水变成烯丙基正离子,通过电荷离域,可以使吲哚环上的
Over the past decade,the organocatalytic enantioselective nitro-Michael addition of ketones or aldehydes to nitroolefins has become an important and powerful tool for the stereocontrolled formation of