- BENZIMIDAZOLE COMPOUNDS AS HDAC6 INHIBITORS
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Novel compounds of Formula I are described, where the compounds are selective HDAC6 inhibitors suitable for treatment of diseases associated with HDAC6, where X, Y, Z, A1, A2, Q1 and Q2 are as described.
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- QUINOXALINE DERIVATIVES
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The present invention relates to compounds according to general formula (I), which act as modulators of the glucocorticoid receptor and can be used in the treatment and/or prophylaxis of disorders which are at least partially mediated by the glucocorticoid receptor.
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Page/Page column 62
(2021/07/24)
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- Synthesis and antileishmanial activity of fluorinated rhodacyanine analogues: The ‘fluorine-walk’ analysis
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In a search for potent antileishmanial drug candidates, eighteen rhodacyanine analogues bearing fluorine or perfluoroalkyl substituents at various positions were synthesized. These compounds were tested for their inhibitory activities against Leishmania martiniquensis and L. orientalis. This ‘fluorine-walk’ analysis revealed that the introduction of fluorine atom at C-5, 6, 5′, or 6′ on the benzothiazole units led to significant enhancement of the activity, correlating with the less negative reduction potentials of the fluorinated analogues confirmed by the electrochemical study. On the other hand, [sbnd]CF3 and [sbnd]OCF3 groups were found to have detrimental effects, which agreed with the poor aqueous solubility predicted by the in silico ADMET analysis. In addition, some of the analogues including the difluorinated species showed exceptional potency against the promastigote and axenic amastigote stages (IC50 = 40–85 nM), with the activities surpassing both amphotericin B and miltefosine.
- Lasing, Thitiya,Phumee, Atchara,Siriyasatien, Padet,Chitchak, Kantima,Vanalabhpatana, Parichatr,Mak, Kit-Kay,Hee Ng, Chew,Vilaivan, Tirayut,Khotavivattana, Tanatorn
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supporting information
(2019/12/09)
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- FURTHER SUBSTITUTED TRIAZOLO QUINOXALINE DERIVATIVES
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The present invention relates to compounds according to general formula (I) which act as modulators of the glucocorticoid receptor and can be used in the treatment and/or prophylaxis of disorders which are at least partially mediated by the glucocorticoid receptor.
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Paragraph 0389-0391
(2020/02/08)
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- KOtBu-Promoted Transition-Metal-Free Transamidation of Primary and Tertiary Amides with Amines
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This work discloses transamidation of primary and tertiary amides with a range of aryl, heteroaryl, and aliphatic amines using potassium tert-butoxide. The reaction proceeds at room temperature under transition-metal-free conditions providing secondary amides in high yields. Moreover, reaction of cyclopropyl amine with tertiary amides proceeds with ring-opening to provide a rapid access to enamides.
- Ghosh, Tridev,Jana, Snehasish,Dash, Jyotirmayee
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supporting information
p. 6690 - 6694
(2019/09/12)
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- Synthesis method and intermediate for 2-bromo-5-fluoro-4-nitroaniline
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The invention discloses a synthesis method and an intermediate for 2-bromo-5-fluoro-4-nitroaniline. The synthesis method for 2-bromo-5-fluoro-4-nitroaniline comprises the step of carrying out a nitration reaction on 2-bromo-5-fluoroaniline and a nitration reagent to generate the 2-bromo-5-fluoro-4-nitroaniline, or comprises the following steps: reacting the 2-bromo-5-fluoroaniline with an amino protection reagent to obtain amino-protected 2-bromo-5-fluoroaniline, then carrying out the nitration reaction on the amino-protected 2-bromo-5-fluoroaniline and the nitration reagent to generate a nitration product that is the intermediate, and finally, removing the amino protection group from the nitration product to obtain the 2-bromo-5-fluoro-4-nitroaniline. The synthesis method has the advantages of high reaction yield, high product purity and easily available raw materials.
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Paragraph 0076; 0077
(2020/01/12)
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- Cobalt(II)-catalyzed regioselective C-H halogenation of anilides
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A cobalt-catalyzed regioselective C-H halogenation methodology is reported herein. The highlight of this work is the highly selective C-H functionalization of anilides, which results in high-yielding, versatile, and practical halogenated products. Thereby, brominations, chlorinations and iodinations of many electron-rich and electron-deficient anilides were achieved in a highly selective fashion. Mechanistic studies with respect to the pathway of the reaction are also described.
- Li, Ze-lin,Sun, Kang-kang,Cai, Chun
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supporting information
p. 5433 - 5440
(2018/08/12)
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- Palladium-Catalyzed, ortho-Selective C-H Halogenation of Benzyl Nitriles, Aryl Weinreb Amides, and Anilides
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A palladium-catalyzed, ortho-selective C-H halogenation methodology is reported herein. The highlight of the work is the highly selective C(sp2)-H functionalization of benzyl nitriles in the presence of activated C(sp3)-H bond, which results in good yields of the halogenated products with excellent regioselectivity. Along with benzyl nitriles, aryl Weinreb amides and anilides have been evaluated for the transformation using aprotic conditions. Mechanistic studies yield interesting aspects with respect to the pathway of the reaction and the directing group abilities.
- Das, Riki,Kapur, Manmohan
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p. 1114 - 1126
(2018/06/18)
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- Mild C - H halogenation of anilides and the isolation of an unusual palladium(I)-palladium(II) species
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Reducing the load: A facile palladium-catalyzed ortho-selective bromination and chlorination of anilides occurs under aerobic conditions at room temperature when N-halosuccinimides (NXS) are used in the presence of p-toluenesulfonic acid (PTSA). The orthopalladated PTSA complex is not only catalytically competent but also undergoes a reductive process to yield an unusual PdI-PdII tetramer (see structure; Pdgreen, Ored, Syellow, Cgray). Copyright
- Bedford, Robin B.,Haddow, Mairi F.,Mitchell, Charlotte J.,Webster, Ruth L.
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supporting information; experimental part
p. 5524 - 5527
(2011/07/31)
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- ONE-POT REDUCTIVE ACETAMIDATION OF ARYL NITRO COMPOUNDS
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The present invention provides a method for the reductive acetamidation of an aryl nitro compound by reacting a substituted acid with an aryl nitro compound and adding a catalytic amount of a base with the substituted acid and the aryl nitro compound to form an acetamidation aryl nitro compound. The acetamidation aryl nitro compound is then purified.
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Page/Page column 9
(2008/06/13)
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