- High Turnover Pd/C Catalyst for Nitro Group Reductions in Water. One-Pot Sequences and Syntheses of Pharmaceutical Intermediates
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Commercially available Pd/C can be used as a catalyst for nitro group reductions with only 0.4 mol % Pd loading. The reaction can be performed using either silane as a transfer hydrogenating agent or simply a hydrogen balloon (μ1 atm pressure). With this technology, a series of nitro compounds was reduced to the desired amines in high chemical yields. Both the catalyst and surfactant were recycled several times without loss of reactivity.
- Gallou, Fabrice,Li, Xiaohan,Lipshutz, Bruce H.,Takale, Balaram S.,Thakore, Ruchita R.
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supporting information
p. 8114 - 8118
(2021/10/25)
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- Palladium(II)-catalyzed, heteroatom-directed, regioselective C-H nitration of anilines using pyrimidine as a removable directing group
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A new palladium-catalyzed, heteroatom-directed strategy for C-H nitration of anilines is described. This C-H functionalization reaction is highly ortho-selective and results in very good yields. The highlight of the work is the use of pyrimidine as the removable directing group. This approach constitutes one of the rare methods of ortho-nitration of anilines, a reaction that is normally very difficult to achieve via traditional approaches.
- Pawar, Govind Goroba,Brahmanandan, Abhilashamole,Kapur, Manmohan
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supporting information
p. 448 - 451
(2016/02/18)
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- UV-absorbers for ophthalmic lens materials
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UV absorbing compounds that are particularly useful in ophthalmic devices are disclosed.
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Page/Page column 7; 8
(2010/10/03)
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- HEAT SHOCK PROTEIN 90 INHIBITORS, METHODS OF PREPARING SAME, AND METHODS FOR THEIR USE
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Novel classes of molecular chaperone Heat shock protein 90 (Hsp90) inhibitors are disclosed. These compounds are useful in treating and preventing cancer and other Hsp90-related diseases and conditions, such as inflammation and neurodegenerative disorders. Methods of treating and preventing cancer and other Hsp90 related diseases and conditions are disclosed that include administering to the subject a therapeutically effective amount of an Hsp90 inhibitor. Methods of preparing the novel Hsp90 inhibitors are also provided.
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Page/Page column 26
(2010/04/28)
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- Benzimidazolinone derivatives
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Benzimidazolinone derivatives of the general formula (I): STR1 wherein R1, R2 and R3, which may be the same or different, each is a hydrogen or halogen atom or a lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, hydroxyl, lower alkoxy, aryloxy, acyl, cyano, carboxyl, a lower alkoxycarbonyl, carbamoyl, nitro or nitrogen-containing 5- or 6-membered heterocyclic group; A is an ethylene group which may optionally have at least one branch; R4 and R5, which may be the same or different, each is a lower alkyl group or R4 and R5, together with the adjacent nitrogen atom, represent a pyrrolidinyl, piperidino or a morpholino group provided that when STR2 is a piperidino or diethylamino group, at least one of R1, R2 and R3 is other than a hydrogen atom, or pharmaceutically acceptable salts thereof, methods of producing the same and pharmaceutical compositions containing the same are disclosed. Pharmacologically, the above compounds (I) have pulmonary surfactant secretion promoting activity.
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- Benzocrown Derivatives as Ionophores for Alkali Cations, II. - Synthesis and Comparison of Urethane-, Ether-, and Ester-Linked Bis-Crown Compounds and Several "Crown-Ring Free" Analogues
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Nitro derivatives of bis-crown ethers with urethane (2), ether (10), and ester (9, 16) linkage not being able to form hydrogen bridges were synthesized, and their K(1+) selectivities were determined.A remarkable effect of the NO2 group on the selectivity was observed when a NO2***NH hydrogen bond could be formed while the others showed only slight improvement in general electroanalytical parameters.Several analogues without the crown ether ring (25, 26) were also prepared, but these compounds lost their alkaline ionophore properties.
- Toeke, Laszlo,Bitter, Istvan,Agai, Bela,Hell, Zoltan,Lindner, Ernoe,et al.
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p. 549 - 554
(2007/10/02)
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- THE NUCLEOPHILIC AROMATIC PHOTOSUBSTITUTIONS OF 4,5-DINITROVERATROLE WITH AMINES. PHOTOREDUCTIONS OF AROMATIC DINITROCOMPOUNDS
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4,5-Dinitroveratrole is effectively photosubstituted by amines with relatively high ionization potential such as methylamine, n-butylamine and ethyl glycinate, but is mainly photoreduced when amines with relatively low ionization potential, such as dimethyl or trimethylamine are used.The photoreduction of several aromatic dinitrocompounds by triethylamine gives nitroanilines.A mechanistic scheme is proposed embracing our photosubstitutions and photoreductions, based on our experimental results and on MINDO/3 calculations of the ground states and the more likely intermediates.
- Marquet, Jorge,Moreno-Manas, Marcial,Vallribera, Adelina,Virgili, Albert,Bertran, Joan,et al.
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p. 351 - 360
(2007/10/02)
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- 4-Methyl-5-(unsubstituted and substituted phenoxy)-6-methoxy-8-(aminoalkylamino)quinolines
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Compounds of the class including 4-methyl-5-(unsubstituted and substitutedhenoxy)-6-methoxy-8-(aminoalkylamino)quinolines as the free bases and pharmaceutically acceptable acid amine salts are described. The compounds are highly effective antimalarial agents which possess, surprisingly, both tissue schizonticidal (radical curative) and blood schizonticidal (suppressive) activity. In addition, these drugs have significantly better therapeutics indices than primaquine which is the current tissue schizonticidal drug of choice. Primaquine possesses no useful blood schizonticidal activity at tolerated dose levels.
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