Department of Chemistry, Indian Institute of Technology Madras, Chennai 600036, India.
J Org Chem. 2021 May 7;86(9):6994-7001. doi: 10.1021/acs.joc.1c00510. Epub 2021 Apr 27.
Commercially available [(PPh)NiCl] was found to be an efficient catalyst for the mono--alkylation of (hetero)aromatic amines, employing alcohols to deliver diverse secondary amines, including the drug intermediates chloropyramine () and mepyramine (), in excellent yields (up to 97%) via the borrowing hydrogen strategy. This method shows a superior activity (TON up to 10000) with a broad substrate scope at a low catalyst loading of 1 mol % and a short reaction time. Further, this strategy is also successful in accessing various quinoline derivatives following the acceptorless dehydrogenation pathway.
市售的[(PPh)NiCl]被发现是一种高效的催化剂，可用于（杂）芳胺的单烷化反应，通过 borrowing hydrogen 策略，醇可作为氢源，将多种仲胺，包括药物中间体氯吡拉敏（）和甲吡拉敏（），高效地转化为相应的产物，产率高达 97%。该方法在 1 mol%的低催化剂负载量和较短的反应时间下，具有优异的活性（TON 高达 10000）和广泛的底物范围。此外，该策略还可成功应用于无受体脱氢途径，得到各种喹啉衍生物。
