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The pipecolic linker—an acid-labile handle for derivatization of secondary amines on a solid-support. Part 3
Journal article   Peer reviewed

The pipecolic linker—an acid-labile handle for derivatization of secondary amines on a solid-support. Part 3

Paweł Zajdel, Nicolas Masurier, Vittorio Canale, Pascal Verdie, Muriel Amblard, Maciej Pawłowski, Jean Martinez and Gilles Subra
Tetrahedron Letters, Vol.54(8), pp.998-1002
02/2013
DOI: https://doi.org/10.1016/j.tetlet.2012.12.036

Abstract

Solid-phase synthesis Pipecolic linker Indole sulfonamide Nitro reduction N-arylation
Herein, we demonstrate the versatility of the pipecolic linker for the structural diversification of secondary amines with potential CNS activity. The solid-phase methods elaborated involved N1-indole sulfonylation, nitroindole and nitroarene reduction, and microwave-assisted Buchwald–Hartwig N-arylation.
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