A convergent strategy for the synthesis of biologically relevant C4-substituted indole scaffolds was demonstrated using Pd(II)-catalyzed remote CÀH functionalization of indoles and azaindoles. The reaction displays high regioselectivity for the C4-position of indole-3-carbaldehydes using glycine as an inexpensive transient directing group. Notable features of this transformation include the selective formation of six-membered palladacyle and excellent functional group tolerance.
pH and solvent sensitive fractal self-assembly of human amylin and fractal characteristics of its aggregates are investigated using different microscopy, laser light scattering, and molecular docking techniques.
The development of a rational strategy for achieving site-selective C4−H halogenation of indoles is an appealing yet challenging task. Herein, we disclose a Pd(II)-catalyzed transient directing group (TDG)-assisted methodology for realizing C4 chlorination/bromination of indoles employing glycine as the TDG and NFSI as a bystanding oxidant. The use of inexpensive and commercially available CuX 2 as the halide source is the key highlight of this protocol. Furthermore, the TDG methodology was also extended to accessing C4 acetoxylated indoles employing acetic acid as the acetate source and 1-fluoro-2,4,6trimethylpyridinium triflate as the oxidant.
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