Mitchell David, Yu Hannah
Eli Lilly & Company, Lilly Research Laboratories, Global Chemical Process Research and Development, Indianapolis, IN 46285, USA.
Curr Opin Drug Discov Devel. 2003 Nov;6(6):876-83.
Synthetic organic chemists have recognized the hydroarylation of alkynes and alkenes as a versatile methodology. In the first part of this review, the regio- and stereochemistry of the hydroarylation of alkynes and the synthetic applications of this reaction in the synthesis of antiviral agents and steroid derivatives will be discussed. In the second part, applications of the hydroarylation of alkenes in the syntheses of epibatidine analogs, argemonine, retinoid X receptor (RXR), retinoic acid receptor (RAR) modulators and neurokinin (NK) receptor NK1 antagonists will be discussed. Emphasis will be placed on the application of Pd-catalyzed hydroarylation to the synthesis of biologically active compounds.
合成有机化学家已认识到炔烃和烯烃的氢芳基化是一种通用方法。在本综述的第一部分,将讨论炔烃氢芳基化的区域化学和立体化学以及该反应在抗病毒剂和甾体衍生物合成中的应用。在第二部分,将讨论烯烃氢芳基化在埃博霉素类似物、精胍菌素、视黄酸X受体(RXR)、维甲酸受体(RAR)调节剂和神经激肽(NK)受体NK1拮抗剂合成中的应用。重点将放在钯催化的氢芳基化在生物活性化合物合成中的应用上。