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Preparation of Disubstituted Phenyl Propargyl Alcohols, their Use in Oxathiolene Oxide Synthesis, and Evaluation of the Oxathiolene Oxide Products as Anticarcinogenic Enzyme Inducers
Letters in Organic Chemistry ( IF 0.7 ) Pub Date : 2009-04-01 , DOI: 10.2174/157017809787893064
Maben Ying 1 , Matthew G Smentek , Rong Ma , Cynthia S Day , Suzy V Torti , Mark E Welker
Affiliation  

A number of alkynols have been prepared by Sonogoshira coupling of propargyl alcohol to disubstituted aromatic halides. Chelation controlled addition of organometallic nucleophiles to these alkynols was then affected followed by the addition of sulfur dioxide. This methodology was used to prepare a number of oxathiolene oxides which have been screened as NQO1 (quinone oxidoreductase) inducers.

中文翻译:

二取代苯基炔丙醇的制备、它们在氧化硫杂环戊烯的合成中的应用以及作为抗癌酶诱导剂的氧化硫杂环硫醇产物的评价

许多炔醇已通过炔丙醇与二取代芳族卤化物的 Sonogoshira 偶联制备。然后通过螯合控制将有机金属亲核试剂添加到这些炔醇中,然后添加二氧化硫。该方法用于制备许多已被筛选为 NQO1(醌氧化还原酶)诱导剂的 oxathiolene 氧化物。
更新日期:2009-04-01
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