163105-90-6Relevant articles and documents
PIPERIDINYL-METHYL-PURINEAMINES AS NSD2 INHIBITORS AND ANTI-CANCER AGENTS
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Page/Page column 59, (2021/02/19)
The present invention provides a compound of Formula (I): (I) or an enantiomer, an enantiomeric mixture, or a pharmaceutically acceptable salt thereof; wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds; and methods of using such compounds for treating a disease or condition mediated by nuclear SET domain-containing protein 2 (NSD2).
Highly efficient one-pot access to functionalized arylboronic acids via noncryogenic bromine/magnesium exchanges
Leermann, Timo,Leroux, Frederic R.,Colobert, Francoise
supporting information; experimental part, p. 4479 - 4481 (2011/10/09)
A general and convenient protocol for the electrophilic borylation of aryl Grignard reagents prepared from arylbromides by direct insertion of magnesium in the presence of LiCl or by Mg/Br exchange with iPrMgCl?LiCl has been developed. Various aryl boronic acids were synthesized in a straightforward manner in excellent yields at 0 °C.
Aryl-and heteroaryl-substituted tetrahydroisoquinolines and use thereof to block reuptake of norepinephrine, dopamine and serotonin
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Page/Page column 17, (2008/06/13)
The present invention relates to a method of treating disorders by administering to a patient in need of such treatment a therapeutically effective amount of a compound of formula (I): wherein R1-R8 are as described herein, R4 being aryl or heteroaryl.
Palladium-catalyzed cross-coupling reactions of pyridylboronic acids with heteroaryl halides bearing a primary amine group: Synthesis of highly substituted bipyridines and pyrazinopyridines
Thompson, Amy E.,Hughes, Gregory,Batsanov, Andrei S.,Bryce, Martin R.,Parry, Paul R.,Tarbit, Brian
, p. 388 - 390 (2007/10/03)
(Chemical Equation Presented). A range of halogenated aromatics and heteroaromatics bearing a primary amine group are shown to be suitable substrates for Suzuki cross-coupling reactions with arylboronic acids and pyridylboronic acids under standard conditions, without the need for protection/deprotection steps. New amino-substituted arylpyridines, bipyridines, and pyrazinopyridines have thereby been obtained. Conditions for the efficient syntheses of 2-methoxy-5-pyridylboronic acid 1 and 2-methoxy-3-pyridylboronic acid 2 in ca. 75 g batches have been defined. A 2-fold reaction of 2-amino-5-bromopyrazine with 2,5-dimethoxy-1,4-benzenediboronic acid affords 1,4-dimethoxy-2,5-bis[2-(5-aminopyrazyl)]benzene 31. The X-ray crystal structures of 1 and 31·DMF are reported.
USING ALKYLMETAL REAGENTS FOR DIRECTED METALATION OF AZAAROMATICS
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Page 8, (2010/02/09)
Substituted alkylmetal reagents such as (trimethylsilylmethyl)lithium are reacted with azaaromatic compounds and/or nitrogen heterocycle compounds to produce functionalized azaaromatic compounds and functionalized nitrogen heterocycle compounds.
New shelf-stable halo- and alkoxy-substituted pyridylboronic acids and their suzuki cross-coupling reactions to yield heteroarylpyridines
Parry, Paul R.,Bryce, Martin R.,Tarbit, Brian
, p. 1035 - 1038 (2007/10/03)
New shelf-stable pyridylboronic acids have been synthesized: bromine-lithium exchange followed by reaction with triisopropylborate (TIPB) yielded 2-fluoro-5-pyridylboronic acid (4), 3-bromo-5-pyridylboronic acid (5) and 2-ethoxy-5-pyridylboronic acid (6);