- DITERPENOID COMPOUNDS THAT ACT ON PROTEIN KINASE C (PKC)
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This present disclosure relates to protein kinase C (PKC) modulating compounds, methods of treating a subject with cancer using the compounds, and combination treatments with a second therapeutic agent.
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Paragraph 0509; 0510
(2021/04/02)
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- Synthesis of Tertiary Benzylic Nitriles via Nickel-Catalyzed Markovnikov Hydrocyanation of α-Substituted Styrenes
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The Markovnikov hydrocyanation of α-substituted styrenes enables the synthesis of tertiary benzylic nitriles under nickel catalysis. The Lewis-acid-free transformation features an unprecedented functional groups tolerance, including the-OH and-NH2 groups. A broad range of tertiary benzylic nitriles were obtained in good to excellent yields. In addition, an asymmetric version of this reaction was preliminarily investigated.
- Xing, Yidan,Yu, Rongrong,Fang, Xianjie
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p. 1008 - 1012
(2020/02/04)
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- Synthesis of indolines by copper-mediated intramolecular aromatic C-H amination
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A Cu(OAc)2-mediated intramolecular aromatic C-H amination proceeds with the aid of a picolinamide-type bidentate coordination group to deliver the corresponding indolines in good yields. The reaction occurs smoothly even under noble-metal-free conditions, and in some cases the use of an MnO2 terminal oxidant renders the process catalytic in Cu. The mild oxidation aptitude of Cu(OAc)2 and/or MnO2 accommodates the formation of electron-rich thiophene-and indole-fused indoline analogues. The Cu-based system can provide an effective approach to various indolines of potent interest in pharmaceutical and medicinal chemistry.
- Takamatsu, Kazutaka,Hirano, Koji,Satoh, Tetsuya,Miura, Masahiro
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p. 3242 - 3249
(2015/03/30)
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- 17a-HYDROXYLASE/C17,20-LYASE INHIBITORS
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The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5, R6, A and n are as defined herein. A deuteriated derivative of the compound of Formula (I) is also provided.
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Paragraph 0440
(2014/03/21)
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- 17α-HYDROXYLASE/C17,20-LYASE INHIBITORS
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The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5, R6, A and n are as defined herein. A deuteriated derivative of the compound of Formula (I) is also provided.
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Page/Page column 72
(2012/04/04)
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- Synthesis of α-Aryl nitriles through palladium-catalyzed decarboxylative coupling of cyanoacetate salts with aryl halides and triflates
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Worth its salt: The palladium-catalyzed decarboxylative coupling of the cyanoacetate salt as well as its mono- and disubstituted derivatives with aryl chlorides, bromides, and triflates is described (see scheme). This reaction is potentially useful for the preparation of a diverse array of α-aryl nitriles and has good functional group tolerance. S-Phos=2-(2,6- dimethoxybiphenyl)dicyclohexylphosphine), Xant-Phos=4,5-bis(diphenylphosphino)- 9,9-dimethylxanthene. Copyright
- Shang, Rui,Ji, Dong-Sheng,Chu, Ling,Fu, Yao,Liu, Lei
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supporting information; experimental part
p. 4470 - 4474
(2011/06/24)
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- Process for Preparing 2-Arylcarbonyl Compounds, 2-Aryl Esters and 2-Arylnitriles and their Heteroaromatic Analogues
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Process for preparing compounds by cross-coupling of enolizable carbonyl compounds, nitriles or their analogues with substituted aryl or heteroaryl compounds in the presence of a Br?nsted base and of a catalyst or precatalyst containing a.) a transition m
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Page/Page column 6
(2008/12/08)
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- Process for preparing benzylnitriles
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A process is described for preparing an aromatic compound substituted by a tertiary nitrile of Formula (1.0.0): comprising treating a substituted aromatic compound of Formula (2.0.0): with a secondary nitrile of Formula (3.0.0): in the presence of a base having a pKanumerical value in the range of from about 17 to about 30, provided that the difference in pKanumerical values between said base and the corresponding tertiary nitrile of Formula (3.0.0) is no more than about 6; in an aprotic solvent having a dielectric constant (∈) of less than about 20; and at a reaction temperature in the range of from about 0° C. to about 120° C.; whereby there is formed said tertiary-nitrile-substituted aromatic compound final product of Formula (1.0.0); wherein the constituent parts W1, W2, W3, W4, and W5; and the substituent moieties R1, R2, R3, R4, R5, R6, and R7in the compounds of Formulas (1.0.0), (2.0.0) and (3.0.0) are selected from known organic groups and radicals as further detailed in the instant specification.
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- 5[W(substituted aryl)alkenylene and alkynylene]-2,4-diaminopyrimidines as pesticides
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5-Substituted-2,4-diaminopyrimidines, and agriculturally acceptable salts thereof, when present in insecticidally or acaricidally effective amounts, and with a suitable agricultural carrier, are useful as active ingredients in novel insecticidal and acaricidal compositions. These pyrimidines may be represented by the following formula: STR1 wherein Ar is STR2 and wherein U is an alkenylene or alkynylene moiety, and R, R1, R2, R3, R4, V, W, X, Y, Z and n are as defined herein; also disclosed and claimed are novel intermediates thereof.
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- 6-substituted-3,5-diamino-1,2,4-triazines as insecticides
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An insecticidal composition comprising, in admixture with an agriculturally acceptable carrier, an insecticidally effective amount of a 1,2,4-triazine compound of the formula STR1 wherein m is 0 to 12; n is 0 or 1; T is CH2, CH=CH, or C C; X is Si(CH3)2, C(CH3)2, CH(CH3), or O; or R is methyl, vinyl, cyclopentyl, phenyl, naphthyl, or a substituted phenyl of the formula: STR2 wherein Q, U, W, Y, Z, and R1, R2, R3, R4 are as defined herein; and methods of using the same.
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