A straightforward approach to N-substituted-2H-indazol-2-amines through reductive cyclization. Issue 16 (19th April 2017)

• Record Type: Journal Article
• Authors: Schoene, Jens; Bel Abed, Hassen; Christmann, Mathias; Nazaré, Marc
• Is Part Of: Tetrahedron letters. Volume 58:Issue 16(2017)
• Page Start: 1633
• Page End: 1635
• Publication Date: 2017-04-19
• Subjects: 2H-Indazole -- Cadogan reaction -- NN bond formation -- Reductive cyclization; Chemistry, Organic -- Periodicals; 547.005
• DOI: 10.1016/j.tetlet.2017.03.031
• Languages: English
• ISSNs: 0040-4039

Abstract

Graphical abstract: Highlights: A two-step, one-pot reaction to access N -substituted-2 H -indazol-2-amine derivatives has been elaborated. A diverse set of analogues was obtained by a sequential in-situ hydrazone formation and reductive cyclization. This allows the rapid generation of "drug-like" compound libraries of novel N -amino heterocycles. Abstract: A versatile two-step, one-pot reaction to access N -substituted-2 H -indazol-2-amine derivatives has been elaborated. A diverse set of analogues was obtained by a sequential hydrazone formation and reductive cyclization in moderate to good yields from readily available starting materials. The strategy tolerates a broad range of substitutions pattern and functional groups allowing further derivatizations.