Jahan Kousar, Sood Mehak, Jain Osheen, Sahoo Subash C, Bharatam Prasad V
Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Sector 67, S. A. S. Nagar, Punjab, India.
Lloyd Institute of Management and Technology, Plot No.-3, Knowledge Park-II, Greater Noida, Uttar Pradesh, India-201306.
Org Biomol Chem. 2024 Sep 11;22(35):7121-7127. doi: 10.1039/d4ob01166j.
In contrast to previously reported free-radical pathways to functionalize imidazo[1,2-]pyridines at the C-5 centre, directing group approaches are rare. Herein, we demonstrate a rhodium(III) catalyzed efficient and regioselective strategy for directed C-5 functionalization of imidazo[1,2-]pyridines using -methoxyamide as a directing group. This methodology facilitates directed arylation without the necessity for pre-functionalization. It also allows for gram-scale synthesis and post-functionalization.
与先前报道的在咪唑并[1,2 -]吡啶的C - 5中心官能团化的自由基途径相反,导向基团方法很少见。在此,我们展示了一种铑(III)催化的高效且区域选择性的策略,该策略使用甲氧基酰胺作为导向基团,对咪唑并[1,2 -]吡啶进行导向C - 5官能团化。这种方法有助于直接进行芳基化,而无需预官能团化。它还允许进行克级规模的合成和后官能团化。