- Iridium-catalyzed silylation of aryl C-H bonds
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A method for the iridium-catalyzed silylation of aryl C-H bonds is described. The reaction of HSiMe(OSiMe3)2 with arenes and heteroarenes catalyzed by the combination of [Ir(cod)(OMe)]2 and 2,4,7-trimethylphenanthroline occurs with the aromatic compound as the limiting reagent and with high levels of sterically derived regioselectivity. This new catalytic system occurs with a much higher tolerance for functional groups than the previously reported rhodium-catalyzed silylation of aryl C-H bonds and occurs with a wide range of heteroarenes. The silylarene products are suitable for further transformations, such as oxidation, halogenation, and cross-coupling. Late-stage functionalization of complex pharmaceutical compounds was demonstrated.
- Cheng, Chen,Hartwig, John F.
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supporting information
p. 592 - 595
(2015/01/30)
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- INTERMOLECULAR C-H SILYLATION OF UNACTIVATED ARENES
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Reaction mixtures for silvlating arene substrates and methods of using such reaction mixtures to silyiate the arene substrates are provided. Exemplary reaction mixtures include the arene substrate, a liganded metal catalyst, a hydrogen acceptor and an organic solvent. The reaction conditions allow for diverse substituents on the arene substrate.
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Paragraph 00192
(2015/03/28)
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- Tetracyclic compounds
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The invention relates to compounds of the general formula I: STR1 or a salt thereof, in which A represents a pyridine ring or a halogen substituted pyridine ring, R1 represents hydrogen, alkyl (1-6 C), alkoxy (1-6 C), alkylthio (1-6 C), halogen, OH, SH or CF3 R2 represents hydrogen or a lower alkyl or aralkyl group and n and m may each be 1, 2 or 3 with the proviso that the sum of m and n must be 2, 3 or 4, having CNS activity, a pronounced antihistamine activity and little or no antiserotonin activity.
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