Premium
Site‐Selective CH Borylation of Quinolines at the C8 Position Catalyzed by a Silica‐Supported Phosphane–Iridium System
Author(s) -
Konishi Shota,
Kawamorita Soichiro,
Iwai Tomohiro,
Steel Patrick G.,
Marder Todd B.,
Sawamura Masaya
Publication year - 2014
Publication title -
chemistry – an asian journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.18
H-Index - 106
eISSN - 1861-471X
pISSN - 1861-4728
DOI - 10.1002/asia.201301423
Subject(s) - borylation , iridium , quinoline , chemistry , catalysis , ligand (biochemistry) , combinatorial chemistry , tetra , antagonist , stereochemistry , medicinal chemistry , organic chemistry , receptor , aryl , biochemistry , alkyl
Site‐selective CH borylation of quinoline derivatives at the C8 position has been achieved by using a heterogeneous Ir catalyst system based on a silica‐supported cage‐type monophosphane ligand SMAP. The efficient synthesis of a corticotropin‐releasing factor 1 (CRF 1 ) receptor antagonist based on a late‐stage CH borylation strategy demonstrates the utility of the C8 borylation reaction.