- Method for preparing N-(5-carboxyl-2-methylphenyl)-4-(3-pyridine)-2-pyrilamine
-
The invention discloses a method for preparing N-(5-carboxyl-2-methylphenyl)-4-(3-pyridine)-2-pyrilamine. The method specifically comprises the following steps: step 1, carrying out ethyl esterification reaction on 3-nitro-4-methyl benzoic acid serving as an initial raw material to generate a compound 2; step 2, reducing nitro of the compound 2 through hydrogenation reduction reaction in the presence of palladium on carbon to generate a compound 3; step 3, reacting the compound 3 with a nitrile amine aqueous solution, and then carrying out base exchange to obtain a compound 4; step 4, carrying out cyclization between the compound 4 and a compound 6 to obtain a compound 7; and step 5, hydrolyzing the compound 7 under the action of an alkaline to generate a compound 8, namely N-(5-carboxyl-2-methylphenyl)-4-(3-pyridine)-2-pyrilamine. The method overcomes the defects that in the prior art such as long reaction time, low yield, high cost, difficulty for industrial production, and the like. A preparation method, which is high in yield, is environmentally-friendly, and is suitable for industrial production, is provided.
- -
-
Paragraph 0029; 0030
(2021/05/05)
-
- Piperlongumine derived cyclic sulfonamides (sultams): Synthesis and in?vitro exploration for therapeutic potential against HeLa cancer cell lines
-
A novel modification of piperlongumine is designed, bearing a cyclic sulphonamide (sultam) and its synthesis is described. For the first time herein we report the synthesis and biological evaluation of the natural product derived cyclic sulfonamides using Grubbs second generation catalyst (Grubbs II) via ring closing metathesis approach. Synthesis of a series of piperlongumine derived sultams is done in a moderate to good yield using Wittig reaction, Ring-Closing Metathesis (RCM) and, amide synthesis by using mixed anhydride, approach. All synthesized compounds were evaluated for anticancer activity and some demonstrated dose dependent reduction in HeLa cell growth. Of these 7, 10 and 14 significantly reduced the cell growth. Consequently their calculated GI50values were found to be 0.1 or 0.1?μM.
- Lad, Nitin P.,Kulkarni, Sarang,Sharma, Rajiv,Mascarenhas, Malcolm,Kulkarni, Mahesh R.,Pandit, Shivaji S.
-
p. 870 - 878
(2016/12/18)
-
- MK2 INHIBITORS AND USES THEREOF
-
The present invention provides compounds, compositions thereof, and methods of using the same.
- -
-
Paragraph 00800; 00824
(2014/10/03)
-
- HETEROCYCLIC COMPOUNDS CONTAINING AN INDOLE CORE
-
Disclosed are novel compounds which inhibit RSK, methods of making such compounds and pharmaceutical compositions comprising such compounds. Also disclosed are methods of treating RSK2 regulated disorders using compounds of the invention.
- -
-
Page/Page column 39-40
(2011/06/26)
-
- Novel potent pyrimido[4,5-c]quinoline inhibitors of protein kinase CK2: SAR and preliminary assessment of their analgesic and anti-viral properties
-
We describe the discovery of novel potent substituted pyrimido[4,5-c] quinoline ATP-competitive inhibitors of protein kinase CK2. A binding model of the inhibitors with the protein was elaborated on the basis of SAR and revealed various modes of interacti
- Pierre, Fabrice,O'Brien, Sean E.,Haddach, Mustapha,Bourbon, Pauline,Schwaebe, Michael K.,Stefan, Eric,Darjania, Levan,Stansfield, Ryan,Ho, Caroline,Siddiqui-Jain, Adam,Streiner, Nicole,Rice, William G.,Anderes, Kenna,Ryckman, David M.
-
scheme or table
p. 1687 - 1691
(2011/05/05)
-
- Synthesis of symmetric diester-functionalised Troeger's base analogues
-
The yields of ester-functionalised Troeger's base analogues are dramatically improved by incorporating an electron-donating group on the aromatic ring and/or enhancing solubil- ity of the aniline unit. In addition to 2,8-diester compounds, 1,7-, 3,9- and 4,10-diester-functionalised Troeger's base analogues have been prepared for the first time.
- Bhuiyan, M. Delower H.,Zhu, Kai-Xian,Jensen, Paul,Try, Andrew C.
-
supporting information; experimental part
p. 4662 - 4670
(2010/10/19)
-
- Pyrazinoindolone inhibitors of MAPKAP-K2
-
Optimization of pyrazinoindolone inhibitors of MAPKAP-K2 (MK2) provides a reasonable balance of cellular potency and physicochemical properties. Mechanistic studies support the inhibition of MK2 which is responsible for the sub-micromolar cellular efficacy.
- Goldberg,Choi,Cogan,Corson,DeLeon,Gao,Gruenbaum,Hao,Joseph,Kashem,Miller,Moss,Netherton,Pargellis,Pelletier,Sellati,Skow,Torcellini,Tseng,Wang,Wasti,Werneburg,Wu,Xiong
-
p. 938 - 941
(2008/09/21)
-
- Anti-Cytokine Heterocyclic Compounds
-
Heterocyclic compounds and analogues thereof and their use as inhibitors of Mitogen-Activated Protein Kinase-Activated Protein kinase-2 (MAPKAP-k2), and also to a method for preventing or treating a disease or disorder that can be treated or prevented by modulating the activity of MAPKAP-K2 in a subject and to pharmaceutical compositions and kits that include these MAPKAP-K2 inhibitors.
- -
-
Page/Page column 32-33
(2010/11/25)
-
- Disubstituted bicyclic heterocycles, the preparations and the use thereof as pharmaceutical compositions
-
New disubstituted bicyclic heterocycles of general formula Ra-A-Het-B-Ar-E (I)Compounds of the above general formula I, wherein E denotes an RbNH-C(=NH)- group, have valuable pharmacological properties, particularly a thrombin-inhibiting effect and the effect of prolonging thrombin time, and those wherein E denotes a cyano group, are valuable intermediates for preparing the other compounds of general formula I. Exemplary compounds of formula I are: (a) 1-Methyl-2-[N-(4-amidinophenyl)-aminomethyl]-benzimidazol-5-yl-carboxylic acid-N-phenyl-N-(2-hydroxycarbonylethyl)-amide, (b) 1-Methyl-2-[N-(4-amidinophenyl)-aminomethyl]-benzimidazol-5-yl-carboxylic acid-N-(2-pyridyl)-N-(hydroxycarbonylmethyl)-amide, (c) 1-Methyl-2-[N-(4-amidino-2-methoxy-phenyl)-aminomethyl]-benzimidazol-5-yl-carboxylic acid-N-(2-pyridyl)-N-(hydroxycarbonylmethyl)-amide, and (d) 1-Methyl-2-[N-[4-(N-n-hexyloxycarbonylamidino)phenyl]aminomethyl]-benzimidazol-5-yl-carboxylic acid-N-(2-pyridyl)-N-(2-ethoxycarbonylethyl) amide.
- -
-
-
- Design of new fluorinated bridged push-pull stilbenes and preparation of LB films for second harmonic generation in the blue domain
-
In order to prepare alternating Y-type multilayers involving push-pull stilbenes giving second harmonic generation (SHG) in the blue domain, we have synthesized two new bridged compounds, 1 and 2, with the hydrophobic chain grafted onto the donor group. The photophysical properties of these dyes in both solution and LB films are reported. The SHG signal of monolayer LB films containing 1 and 2 are close to that of the analog 3 and 4 having the hydrophobic chain grafted onto the acceptor group. Finally, multilayer LB films based on one, two and four bilayers of 1/3 or 2/4 were prepared and the SHG measurements show a regular noncentrosymmetric arrangement for 2/4 films only.
- Desrousseaux,Bennetau,Morand,Mingotaud,Letard,Montant,Freysz
-
p. 977 - 985
(2007/10/03)
-
- Synthesis and properties of an optically active helical bis-cobaltocenium ion
-
The optically active helical bis-cobaltocenium salt 6 is synthesized, as are two related monocobaltocenium salts, 29 and 30. The structure of 6 is analyzed by X-ray diffraction, which shows that the metals are separated by 8.49 ?. Reducing 6 either electrochemically or with K(Hg) produces species that absorb near 920 nm, but the absorption is not an intervalence transition. It originates instead from isolated Co(II) centers. This is demonstrated by the reduction product of 29, which has only one cobalt, also absorbing at a similar wavelength (λmax, = 957 nm). The optical and ESR spectra imply that the unpaired electron in monoreduced 6 is largely localized on cobalt and that direduced 6 is essentially a Co(II)Co(II) diradical. The difference between two Co(III)/Co(II) reduction potentials of 6, 130 mV, is shown to be appropriate for a conjugated dimetallocene with metals so distant. Crystal data for 6: M = 1275.02; orthorhombic, space group P212121; Z = 4; a = 11.560(4), b = 12.244(3), and c = 41.349(17) ?; V = 5852.5 ?3; R = 0.1137 for 4653 reflections having Fo ≥ nσ(Fo) (n = 7.5).
- Gilbert, Adam M.,Katz, Thomas J.,Geiger, William E.,Robben, Matthew P.,Rheingold, Arnold L.
-
p. 3199 - 3211
(2007/10/02)
-