- QUINUCLIDINONE ANALOGUES AS ANTICANCER AGENTS
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The disclosure includes compounds of Formula (I) and Formula(A) wherein R1, R2, R3, m, n, k, and L are defined herein. Also disclosed are methods for treating a neoplastic disease, autoimmune disease, or an inflammatory disorder with these compounds.
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Page/Page column 91-92
(2021/08/13)
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- HETEROCYCLIC COMPOUNDS AS KINASE INHIBITORS, COMPOSITIONS COMPRISING THE HETEROCYCLIC COMPOUND, AND METHODS OF USE THEREOF
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The present disclosure provides a compound of Formula (I) and/or a stereoisomer, a tautomer, a stable isotope, or a pharmaceutically acceptable salt thereof; and therapeutic uses of these compounds. They are kinase inhibitors potentially useful in the tre
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Page/Page column 47
(2020/01/10)
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- Efficient copper-catalyzed trifluoromethylation of aromatic and heteroaromatic iodides: The beneficial anchoring effect of borates
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Efficient copper-catalyzed trifluoromethylation of aromatic iodides was achieved with TMSCF3 in the presence of trimethylborate. The Lewis acid was used to anchor the in situ generated trifluoromethyl anion and suppress its rapid decomposition. Broad applicability of the new trifluoromethylating reaction was demonstrated in the functionalization of different aromatic and heteroaromatic iodides.
- Gonda, Zsombor,Kovacs, Szabolcs,Weber, Csaba,Gati, Tamas,Meszaros, Attila,Kotschy, Andras,Novak, Zoltan
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supporting information
p. 4268 - 4271
(2014/09/30)
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- PROCESS FOR THE PREPARATION OF 2-TRIFLUOROMETHYL ISONICOTINIC ACID AND ESTERS
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The invention relates to a novel process for the preparation of 2- trifluoromethyl isonicotinic acid and esters of the formula I which involves a palladium catalysed carbonylation or cyanation step wherein R1 is hydrogen or Q1-6-alkyl. The 2-trifluoromethyl isonicotinic acid and esters of the formula I are versatile intermediates for the preparation of active pharmaceutical and agrochemical agents such as for instance TAAR 1 agonists of the formula III.
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- SUBSTITUTED PYRAZOLOQUINAZOLINONES AND PYRROLOQUINAZOLINONES AS ALLOSTERIC MODULATORS OF GROUP II METABOTROPIC GLUTAMATE RECEPTORS
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The present invention relates to the pyrazoloquinazolinone and pyrroloquinazolinone derivatives of the general formula (I), as well as pharmaceutical compositions containing them, and their use in the treatment and/or prophylaxis of conditions associated with altered glutamatergic signalling and/or functions, and/or conditions which can be affected by alteration of glutamate level or signalling in mammals, in particular their use in the treatment and/or prophylaxis of acute and chronic neurological and/or psychiatric disorders.
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Page/Page column 149
(2014/01/07)
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- The direct metalation and subsequent functionalization of trifluoromethyl-substituted pyridines and quinolines
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Depending on the choice of the reagent, 2-(trifluoromethyl)-pyridine can be selectively metalated and subsequently carboxylated of otherwise functionalized either at the 3- or at the 6-position. "Optional site selectivity" can also be achieved with 4-(trifluoromethyl)pyridine, which may be deprotonated either at the 2- or at the 3-position. In contrast, 3-(trifluoromethyl)pyridine undergoes nucleophilic addition and ensuing decomposition whatever the base. Depending on the reaction conditions, 2-(trifluoromethyl)quinoline displays reactivity toward lithium reagents at its 3-, 4-, or 8-positions, 3-(trifluoromethyl)quinolines at the 2- or 4-positions, and 4-(trifluoromethyl)quinoline at the 2- or 3-positions. It was therefore possible to prepare four trifluoromethyl-substituted pyridinecarboxylic acids (1, 4, 9, and 10) and six trifluoromethyl-substituted quinolinecarboxylic acids (11, 13, 14, 15, 17, and 18) regioisomerically uncontaminated and in a most straightforward way. ( Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2003).
- Schlosser, Manfred,Marull, Marc
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p. 1569 - 1575
(2007/10/03)
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