Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research , Sector 67, SAS Nagar, Punjab 160 062, India.
J Org Chem. 2013 Nov 1;78(21):10954-9. doi: 10.1021/jo401934q. Epub 2013 Oct 18.
An efficient, microwave-assisted direct C-H arylation at the C-5 position of fully protected L-histidine has been achieved via a palladium-catalyzed transformation reaction. This highly regioselective reaction has been applied to synthesize a series of protected 5-aryl-L-histidines using aryl iodides as coupling partners, in good to excellent yields. The reaction is compatible with substrates possessing electron-donating or electron-withdrawing substituents and offers high reactive functional group tolerance.
通过钯催化转化反应，实现了在完全保护的 L-组氨酸的 C-5 位的高效、微波辅助的直接 C-H 芳基化。该高区域选择性反应已被应用于使用芳基碘化物作为偶联试剂合成一系列保护的 5-芳基-L-组氨酸，产率良好至优秀。该反应与具有供电子或吸电子取代基的底物兼容，并具有高反应官能团耐受性。
