142404-84-0Relevant articles and documents
ADAMANTYL DERIVATES AS P2X7 RECEPTOR ANTAGONISTS
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Page/Page column 155-156, (2010/10/20)
The invention provides compounds of formula (I) pharmaceutically acceptable salt or solvate thereof, in which R1, A1, m and A are as defined in the specification; a process for their preparation; pharmaceutical compositions containin
2-Ethoxy-3-pyridylboronic acid: A versatile reagent for the synthesis of highly-functionalised 3-aryl/heteroaryl-pyridines via Suzuki cross-coupling reactions
Thompson, Amy E.,Batsanov, Andrei S.,Bryce, Martin R.,Saygili, Nezire,Parry, Paul R.,Tarbit, Brian
, p. 5131 - 5135 (2007/10/03)
This paper describes the commercially-viable synthesis and isolation of 2-ethoxy-3-pyridylboronic acid on a ca. 70 g scale via a directed ortho-metalation reaction on readily-available 2-ethoxypyridine. A range of efficient cross-coupling reactions of 2-ethoxy-3-pyridylboronic acid with selected aryl/heteroaryl halides under palladium-catalysed Suzuki-Miyaura conditions yield novel 2-ethoxy-3-aryl/heteroaryl-pyridines in high yield (heteroaryl=pyridyl, pyrimidyl, pyrazyl). The X-ray crystal structure of 2-ethoxy-3-pyridylboronic acid reveals that the boronic acid group takes part in an intramolecular O-H?O bond with the adjacent ethoxy substituent, and an intermolecular O-H?N bond.
N-bromosuccinimide reactions of some heterocycles in the presence or absence of water: An overview of ring versus side chain bromination for the synthesis of important brominated heterocyclic synthons
Goswami,Ghosh,Mukherjee,Avijit Kumar Adak,Ajit Kumar Mahapatra
, p. 173 - 178 (2007/10/03)
Reactions of various heterocycles 1-6 with N-bromosuccinimide in the presence or absence of water have been studied for side chain versus ring bromination to afford some new and important heterocyclic synthons. Interestingly, the N-bromosuccinimide reaction in the presence of perchloric acid, a new condition, affords exclusively the new dibromo aminopicoline 1f, which is not obtained by other presently studied methods.