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Solid-phase Synthesis of [4.4] Spirocyclic Oximes
Published on: February 6, 2019
基地推广的单三组分脱硫交叉合获得4-胺醇
Jiangwei Wen1, Ting Zeng1, Kelu Yan1
1Key Laboratory of Green Natural Products and Pharmaceutical Intermediates in Colleges and Universities of Shandong Province, School of Chemistry and Chemical Engineering, Qufu Normal University, P. R. China. wenjy@qfnu.edu.cn.
一种新方法有效地合成4-胺醇衍生物,使用一,三组合交叉合反应. 这种可扩展的方法提供了高产量,并简化了净化,使其非常适合工业用途.
科学领域:
- 有机化学 有机化学
- 合成化学 合成化学
背景情况:
- 伊米达衍生物在制药和材料科学中至关重要.
- 功能化伊米达的高效合成仍然是一个挑战.
研究的目的:
- 开发一种新的,可扩展的,单合成4 - 胺醇衍生物.
- 建立一个基质介导脱硫交叉合战略.
主要方法:
- 一个一,三组分反应,涉及脱硫交叉合.
- 使用易于获得的起始材料和基础介质.
- 通过简单的过隔离,避免列色谱.
主要成果:
- 成功合成了超过35个4-胺醇衍生物的例子.
- 取得的收益率始终超过85%.
- 已证明可扩展性高达10mmol,产率高达87%.
结论:
- 报告的协议提供了一个简单而有效的途径,以4-cyanoimidazole衍生物.
- 该方法的可扩展性和简化净化强调了其工业适用性.
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