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用于一步合成螺氧杂环丁烷骨架的乙烯基锍试剂
螺氧杂环丁烷骨架是张力杂环,引入目标化合物后,对其刚性,亲水性,氢键接受性产生很大影响1)。因此,氧杂环丁烷合成试剂在药物开发研究中越来越受到关注。
二新戊基乙烯基锍三氟甲磺酸盐 (1)与易得到的醇在光氧化还原条件下,通过氢原子转移(HAT)和加成-消除过程,合成氧杂环丁烷2)。1可用于一步合成通常传统方法难以获得的氧杂环丁烷,且便于在后期阶段将氧杂环丁烷骨架引入到药物中。因此,1有助于研发过程中分子结构的多样化。
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- 1) Oxetanes: Recent Advances in Synthesis, Reactivity, and Medicinal Chemistry
- 2) Oxetane Synthesis via Alcohol C−H Functionalization