- COMPOUNDS, COMPOSITIONS AND METHODS OF USE
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Herein, compounds, compositions and methods for modulating inclusion formation and stress granules in cells related to the onset of neurodegenerative diseases, musculoskeletal diseases, cancer, ophthalmological diseases, and viral infections are described.
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Page/Page column 97-98
(2020/07/06)
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- Process for synthesizing m-isobutylaniline
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The invention relates to a process for synthesizing m-isobutylaniline. According to the invention, isobutyraldehyde and morpholine are used as starting materials and p-toluenesulfonic acid is used as a catalyst to synthesize 2-methyl-1-m-morpholinylpropylene; then 2-methyl-1-m-morpholinylpropylene and nitrobenzoyl chloride are subjected to condensation and hydrolysis, and then an aldehyde group is removed under the action of hydrochloric acid, so m-nitrophenylisobutyl ketone is synthesized; then m-aminophenylisobutyl ketone is synthesized through selective hydrogenation; and finally, m-isobutylaniline is synthesized through a Huang Minglong reaction.
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Paragraph 0011; 0012; 0013
(2018/04/01)
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- Production of [...] (by machine translation)
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Useful as an intermediate for the production of a horticultural [to] acaricidal agent can provide an industrially advantageous method for producing 3 - [...]. [Solution] nitro bromobenzene isobutene and the like, a palladium catalyst, a phosphine-based coordination, bases, solvents, and the auxiliary agent in the presence of reaction, isobutene was added to compound, the additional compound is isolated or not isolated, hydrogenation (catalytic reduction) by the production method 3 - [...] or salts thereof. [Drawing] no (by machine translation)
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- Functional group tolerant Kumada-Corriu-Tamao coupling of nonactivated alkyl halides with aryl and heteroaryl nucleophiles: Catalysis by a nickel pincer complex permits the coupling of functionalized Grignard reagents
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A nickel(II) pincer complex [(MeNN2)NiCl] (1) catalyzes Kumada-Corriu-Tamao cross coupling of nonactivated alkyl halides with aryl and heteroaryl Grignard reagents. The coupling of octyl bromide with phenylmagnesium chloride was used as a test reaction. Using 3 mol % of 1 as the precatalyst and THF as the solvent, and in the presence of a catalytic amount of TMEDA, the coupling product was obtained in a high yield. The reaction conditions could be applied to cross coupling of other primary and secondary alkyl bromides and iodides. The coupling is tolerant to a wide range of functional groups. Therefore, alkyl halides containing ester, amide, ether, thioether, alcohol, pyrrole, indole, furan, nitrile, conjugated enone, and aryl halide moieties were coupled to give high isolated yields of products in which these units stay intact. For the coupling of ester-containing substrates, O-TMEDA is a better additive than TMEDA. The reaction protocol proves to be efficient for the coupling of Knochel-type functionalized Grignard reagents. Thus aryl Grignard reagents containing electron-deficient and/or sensitive ester, nitrile, amide, and CF3 substituents could be successfully coupled to nonactivated and functionalized alkyl iodides. The catalysis is also efficient for the coupling of alkyl iodides with functionalized heteroaryl Grignard reagents, giving rise to pyridine-, thiophene-, pyrazole-, furan-containing molecules with additional functionalities. Concerning the mechanism of the catalysis, [(MeNN2)Ni-(hetero)Ar] was identified as an intermediate, and the activation of alkyl halides was found to take place through a radical-rebound process.
- Vechorkin, Oleg,Proust, Valerie,Hu, Xile
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supporting information; experimental part
p. 9756 - 9766
(2011/03/19)
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- NEW CARBONYLATED (AZA)CYCLOHEXANES AS DOPAMINE D3 RECEPTOR LIGANDS
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The invention relates to compounds of the general formula (I): to the process for preparing them, and to the use thereof as a therapeutic agent.
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Page/Page column 90
(2008/06/13)
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- INDOLE DERIVATIVES AND THEIR USE FOR TESTOSTERONE 5-ALPHA-REDUCTASE-MEDIATED DISEASES
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Indole derivatives of the formula and pharmaceutical compositions thereof. They are useful for treating or preventing testosterone 5-alpha-reductase-mediated diseases, such as alopecia, acnes and prostatism
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