A Convenient Method for the Preparation of 5-, 6- and 7-Azaindoles and Their Derivatives
作者:David Hands、Brian Bishop、Mark Cameron、John S. Edwards、Ian F. Cottrell、Stanley H. B. Wright
DOI:10.1055/s-1996-4312
日期:1996.7
The directed ortho lithiation of 2-tert-butoxycarbonylamino-3-methylpyridine (6a) has provided a convenient method for the preparation of 1H-pyrrolo[2,3-b]pyridine (4a, 7-azaindole). This procedure has been used to prepare a range of 3-substituted 2-tert-butoxycarbonylaminopyridines 6, 2- and 3-substituted and 2,3-disubstituted 1H-pyrrolo[2,3-b]pyridines 4 and shown to be of value in the preparation of 1H-pyrrolo[3,2-c]pyridine (15, 5-azaindole) and 1H-pyrrolo[2,3-c]pyridine (18, 6-azaindole) and derivatives.
2-叔丁氧基羰基氨基-3-甲基吡啶(6a)的直接邻位锂化为制备1H-吡咯并[2,3-b]吡啶(4a,7-氮杂吲哚)提供了一种简便的方法。该程序已用于制备一系列 3-取代的 2-叔丁氧基羰基氨基吡啶 6、2-和 3-取代以及 2,3-二取代的 1H-吡咯并[2,3-b]吡啶 4 并显示出有价值用于制备1H-吡咯并[3,2-c]吡啶(15, 5-氮杂吲哚)和1H-吡咯并[2,3-c]吡啶(18, 6-氮杂吲哚)及其衍生物。