Atom-economic threefold cross-couplings of triarylbismuth reagents with 2-halobenzaldehydes and pot-economic in situ Wittig functionalizations with phosphonium salts
作者:Maddali L. N. Rao、Ritesh J. Dhanorkar
DOI:10.1039/c4ra13348j
日期:——
In this paper we report an efficient pot-economic methodology for the synthesis of ortho-olefinated biaryls. This has been achieved through an atom-economic threefold cross-coupling of triarylbismuth reagents with 2-halobenzaldehydes followed by pot-economic in situ Wittig olefination. The overall process is a pot-economic straightforward synthesis of ortho-olefinated biaryls from 2-halobenzaldehydes, triarylbismuth reagents and phosphonium salts. This pot-economic approach was applied to the formal synthesis of medicinally important Eupomatilone-6.
本文报道了一种高效的原位Wittig烯化反应方法,用于合成邻烯基联苯。通过三芳基铋试剂与2-卤代苯甲醛的三重交叉偶联,继而进行原位Wittig烯化,实现了这一目标。整个过程是从2-卤代苯甲醛、三芳基铋试剂和膦盐出发,高效简便地合成邻烯基联苯。这一方法已成功应用于重要的药用成分Eupomatilone-6的正式合成中。