A Rapid and Efficient Sonogashira Protocol and Improved Synthesis of Free Fatty Acid 1 (FFA1) Receptor Agonists
A Rapid and Efficient Sonogashira Protocol and Improved Synthesis of Free Fatty Acid 1 (FFA1) Receptor Agonists
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DOI：
10.1021/jo902533p
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发表时间：
2010-02-19
影响因子：
3.6
通讯作者：
Ulven, Trond
中科院分区：
文献类型：
--
作者：
Christiansen, Elisabeth;Due-Hansen, Maria E.;Ulven, Trond
使用 2-(二叔丁基膦)-N-苯基吲哚 (cataCXium PIntB) 作为 TMEDA 和水中的配体，开发了一种快速有效的 Pd/Cu 催化芳基溴化物和碘化物与末端炔烃偶联的方案。新方案成功偶联了在标准 Sonogashira 条件下失败的底物，并实现了从 3-(4-溴苯基)-丙酸游离脂肪酸 1 (FFA1) 受体配体的有效通用合成路线。
A protocol for rapid and efficient Pd/Cu-catalyzed coupling of aryl bromides and iodides to terminal alkynes has been developed with use of 2-(di-tert-butylphosphino)-N-phenylindole (cataCXium PIntB) as ligand in TMEDA and water. The new protocol successfully couples substrates which failed with standard Sonogashira conditions, and enables an efficient general synthetic route to free fatty acid 1 (FFA1) receptor ligands from 3-(4-bromophenyl)-propionic acid.