Ligandless microwave-assisted Pd/Cu-catalyzed direct arylation of oxazoles
Ligandless microwave-assisted Pd/Cu-catalyzed direct arylation of oxazoles
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DOI：
10.1021/jo7027135
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发表时间：
2008-04-18
影响因子：
3.6
通讯作者：
Piguel, Sandrine
中科院分区：
文献类型：
--
作者：
Besselievre, Francois;Mahuteau-Betzer, Florence;Piguel, Sandrine
研究了微波辅助钯/铜催化下恶唑与溴代芳烃的直接芳基化反应。该方法是官能团耐受的，并且以良好的产率提供了快速获得药用相关化合物的途径。耦合到货车Leusen恶唑环合成，这种方法是说明了一个方便的两步合成的四个2，5-二芳基恶唑生物碱texamine，texaline，balsoxin，和O-Me-halfordinol从市售的原料。
An efficient microwave-assisted palladium/copper co-mediated direct arylation of oxazoles with aryl bromides under ligandless conditions has been developed. The method is functional group tolerant and provides rapid access to medicinally relevant compounds in good yields. Coupled to the van Leusen oxazole ring synthesis, this methodology is illustrated by an expedient two-step synthesis of the four 2,5-diaryloxazole alkaloids texamine, texaline, balsoxin, and O-Me-halfordinol from commercially available starting materials.