- Intramolecular Pd-catalyzed reductive amination of enolizable sp3-C-H bonds
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A palladium-catalyzed reductive cyclization of nitroarenes has been designed to construct sp3-C-NHAr bonds from sp3-C-H bonds by using an enolizable nucleophile to intercept a nitrosoarene intermediate. Exposure of ortho-substituted nitroarenes to 5 mol ?% of Pd(OAc)2 and 10 mol ?% of phenanthroline under 2 atm of CO constructs partially saturated 5-, 6-, or 7-membered N-heterocycles using α-pyridyl carboxylates, malonates, 1,3-dimethylbarbituric acid, 1,3-diones, or difurans as the nucleophile.
- Ford, Russell L.,Alt, Isabel,Jana, Navendu,Driver, Tom G.
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supporting information
p. 8827 - 8831
(2019/10/28)
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- Synthesis of Aryl-Substituted 3,3a,4,5-Tetrahydropyrrolo[1,2- A [ quinolin-1(2 H)-ones and 2,3,4,4a,5,6-Hexahydro-1 H-pyrido[1,2- A [quinolin-1-ones
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A new route to the title benzo-fused angular tricyclic amides 3,3a,4,5-tetrahydropyrrolo- A nd 2,3,4,4a,5,6-hexahydro-1 H-pyrido[1,2- A [quinolin-1-ones is reported from 1-(tert-butyl) 6-ethyl 3-oxohexanedioate and 1-(tert-butyl) 7-ethyl 3-oxoheptanedioate. Alkylation of these β-keto diesters with a series of 2-nitrobenzyl bromides followed by acid hydrolysis and decarboxylation gives ethyl 6-(2-nitrophenyl)-4-oxohexanoates and ethyl 7-(2-nitrophenyl)-5-oxoheptanoates, respectively. Reductive amination under hydrogenation conditions followed by ester hydrolysis and condensative ring closure affords the final lactam products. The reactions proceed cleanly and only two chromatographic purifications are required.
- Watts, Field M.,Bunce, Richard A.
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p. 564 - 572
(2019/01/10)
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- JAK2 AND ALK2 INHIBITORS AND METHODS FOR THEIR USE
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Compounds having activity as inhibitors of ALK2 kinase and/or JAK2 kinase are disclosed. The compounds have the following structure (I): [FORMULA SHOULD BE INSERTED HERE] including stereoisomers, tautomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, X, z and A are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
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Page/Page column 75
(2014/10/04)
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- Rh2(II)-catalyzed selective aminomethylene migration from styryl azides
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Rh2(II)-Carboxylate complexes were discovered to promote the selective migration of aminomethylenes in β,β-disubstituted styryl azides to form 2,3-disubstituted indoles. Mechanistic data are also presented that suggest that the migration occurs stepwise before diffusion of the iminium ion.
- Kong, Chen,Jana, Navendu,Driver, Tom G.
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supporting information
p. 824 - 827
(2013/03/29)
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- SUBSTITUTED 1H-INDAZOL-1-OL ANALOGS AS INHIBITORS OF BETA CATENIN/TCF PROTEIN-PROTEIN INTERACTIONS
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In one aspect, the invention relates to substituted lH-benzo[d][l,2,3]triazol-l-ol analgoues, derivatives thereof, and related compound; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders, e.g. various tumors and cancers, associated with β-catenin/Tcf protein- protein interaction dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
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Paragraph 00273
(2013/08/28)
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- Benzimidazole derivatives
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A benzimidazole derivative or its medically acceptable salt, represented by the following formula (1), that is a human chymase activity inhibitor capable of being applied clinically: 1wherein, R1 and R2 represent a hydrogen atom, an alkyl group or an alkoxy group, etc., A represents an alkylene group or an alkenylene group, E represents —COOR3, —SO3R3, —CONHR3 or —SO2NHR3, etc., G represents an alkylene group, M represents a single bond or —S(O)m. J represents a heterocyclic group, and X represents —CH= or a nitrogen atom.
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- Solvent free tetrahydropyranylation of alcohols and phenols over sulfuric acid adsorbed on silica gel
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Alcohols and phenols are tetrahydropyranylated in the presence of sulfuric acid adsorbed on silica gel in high to excellent yields in solvent free conditions and is expedited by microwave irradiation. Addition of methanol performs the complete deprotection.
- Heravi, Majid M.,Ajami, Dariush,Ghassemzadeh, Mitra
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p. 1013 - 1016
(2007/10/03)
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- Sulphuric acid adsorbed on silica gel: An efficient catalyst for the protection and deprotection of alcohols with dihydropyran
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Alcohols are tetrahydropyranylated in the presence of sulphuric acid adsorbed on silica gel in dichloromethane in good to excellent yields. Addition of methanol brings about the complete deprotection.
- Heravi,Bigdeli,Nahid,Ajami
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p. 1285 - 1286
(2007/10/03)
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- 5, 10-Dihydroimidazo[2,1-b]quinazolines and pharmaceutical compositions containing them
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A 5,10-dihydroimidazo[2,1-b]quinazoline in which at least one ring carbon atom, other than the carbon atom in the 2-position, bears a substituent, or a pharmaceutically acceptable acid addition salt thereof is a useful cardiotonic agent and vasodilator in heart insufficiency and a blood platelet aggregation inhibitor.
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