- (AZA)INDAZOLYL-ARYL SULFONAMIDE AND RELATED COMPOUNDS AND THEIR USE IN TREATING MEDICAL CONDITIONS
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The invention provides (aza)indazolyl-aryl sulfonamide and related compounds, pharmaceutical compositions, and their use in the treatment of medical conditions, such as cancer, and in inhibiting GCN2 activity.
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Paragraph 0422
(2020/10/21)
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- Synthesis of a series of iridium complexes bearing substituted 2-pyridonates and their catalytic performance for acceptorless dehydrogenation of alcohols under neutral conditions
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A series of Cp*Ir complexes bearing 5- and 4,5-substituted 2-pyridonate ligands have been synthesized and their catalytic performance for acceptorless dehydrogenation of alcohols has been investigated under neutral conditions. Electron-withdrawing groups such as methoxycarbonyl, trifluoromethyl, cyano, and nitro groups at the 5-position promoted the acceptorless dehydrogenation of 1-phenylethanol, whereas electron-donating methyl group at the 5-position retarded the reaction. Furthermore, introduction of methyl group at the 4-position improved the catalytic performance. Thus, Cp*Ir(5-trifluoromethyl-4-methyl-2-pyridonate)Cl (2bc) exhibited the highest catalytic performance among the complexes examined, and also showed good catalytic performance for acceptorless dehydrogenation of primary alcohols.
- Yamaguchi, Ryohei,Kobayashi, Daiki,Shimizu, Mineyuki,Fujita, Ken-ichi
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supporting information
p. 14 - 19
(2017/05/19)
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- Practical synthesis of (6-chloro-3-pyridyl)methylamine by highly selective hydrogenation of 6-chloro-3-pyridinecarbonitrile with improved Raney nickel catalyst
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A practical synthesis of (6-chloro-3-pyridyl)methylamine (1), one of the key intermediates of neo-nicotinoid insecticides, by a highly selective hydrogenation of 6-chloro-3-pyridinecarbonitrile (4) is described. The use of an improved Raney nickel catalyst, prepared from an alloy of low nickel content (Ni 38%, A1 62%) and subjected to heat treatment in water (98 °C, 2 h) after leaching of aluminum, was highly effective for the selective hydrogenation of 4. The hydrogenation of 4 using this catalyst was carried out in EtOH-H2O [6:1 (v/v)] and NH3 at 50 °C and 1.2-1.4 kg cm-2 hydrogen pressure to give 1 in 86% yield and 3-pyridylmethylamine, a dechlorinated by-product, in 2% yield.
- Tanaka, Ken,Nagasawa, Minoru,Sakamura, Hideki
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p. 1227 - 1231
(2007/10/03)
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