- Synthesis of C-14 and C-13, H-2-labeled IKK inhibitor: [14C] and [13C4,D3]-N-(6-chloro-7-methoxy-9H-pyrido3,4- blindol-8-yl)-2-methyl-3-pyridinecarboxamide
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[14C]-N-(6-Chloro-7-methoxy-9H-pyrido [3,4-b]indol-8-yl)-2- methyl-3-pyridinecarboxamide (5B), an IKK inhibitor, was synthesized from [ 14C]-barium carbonate in two steps in an overall radiochemical yield of 41%. The intermediate, [carboxyl-14C]-2-methylnicotinic acid, was prepared by the lithiation and carbonation of 3-bromo-2-methylpyridine. [ 13C4,D3]-N-(6-chloro-7-methoxy-9H-pyrido[3,4-b] indol-8-yl)-2-methyl-3-pyridinecarboxamide (5C) was synthesized from [1,2,3,4-13C4]-ethyl acetoacetate and [D 4]-methanol in six steps in an overall yield of 2%. [ l3C4]-2-methylnicotic acid, was prepared by condensation of [13C4]-ethyl 3-aminocrotonate and acrolein, followed by hydrolysis with lithium hydroxide. Copyright
- Li, Yuexian,Plesescu, Mihaela,Prakash, Shimoga R.
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- Preparation method of 2-4- dibromopyridine-pyridine-formaldehyde (by machine translation)
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The method has the, beneficial effects that the process control temperature. 2 - is lower than-20 DEG C,(1)2 - 2 - 2 - 90 - 120min, 20 °C, 45 - 60min, 20 °C 1h,(2)2 . (by machine translation)
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Paragraph 0013; 0016-0017; 0019-0020; 0023-0024
(2020/01/25)
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- A 2 - bromo -4 - pyridylaldehyde preparation method (by machine translation)
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The invention belongs to the field of organic synthesis, in particular relates to a 2 - bromo - 4 - pyridylaldehyde preparation method, comprises the following steps: (1) 2 - bromo - 4 - methyl pyridine preparation: will be hydrobromic arranged in four bottle, added under mixing 2 - amino - 4 - methylpyridine, to be 2 - amino - 4 - methyl pyridine completely after dissolving, cooling to - 20 °C, slow [...], dropping process control temperature is - 20 °C - - 15 °C; dropped stirring for 90 - 120 min, then dropping sodium nitrite solution, after adding, the temperature to 20 °C, stirring 45 - 60 min and then cooling to - 20 °C - - 25 °C, sodium hydroxide solution, dropping process control temperature is lower than - 15 °C - - 10 °C; after adding, the temperature is raised to 20 °C and stirring 1 h, extraction, the combined organic phase, washing, drying, concentration; (2) 2 - bromo - 4 - pyridylaldehyde preparation. The beneficial effect of the invention is: mild reaction conditions, is easy to operate, after treatment is simple, and easy to enlarge production, is extremely suitable for industrial production; high yield, low prices of raw materials, the production cost is low. (by machine translation)
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Paragraph 0017; 0019; 0020; 0024
(2019/05/28)
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- PROTEASE ACTIVATED RECEPTOR 2 (PAR2) ANTAGONISTS
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A compound of formula (I) or a pharmaceutically acceptable salt, solvate, hydrate thereof (I) Wherein Y, Z, R3, U, R4, m and n are as defined in the claims.
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Page/Page column 47
(2012/08/08)
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- Complexes of 4- and 5-bromo derivatives of 2-(hydroxymethyl)pyridine with copper(II) and cobalt(II) salts. Synthesis and X-ray crystal structures
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Four copper(II) complexes (1-4) and a cobalt(II) complex (5) derived from 4-bromo-2-(hydroxymethyl)pyridine (L1) or 5-bromo-2-hydroxymethyl)pyridine (L2) with Cu(NO3)2·3H2O, CuCl2·2H2O and CoCl2·6H2O have been synthesized and their respective crystal structures studied. They show specific influences owing to the different kind of metal cations and counter anions, the hydration as well as the different position of the bromine substitution on both the coordination of the complex unit and the network structure of the crystal lattice. The Cu(II) complexes of L1 are five-coordinate [Cu(L1)2NO3]NO3·H2O (1) and [Cu(L1)2Cl]Cl·H2O (2) species with distorted quadratic pyramidal and trigonal bipyramidal coordination geometries of the N2O3 and N2O2Cl donor atoms around the Cu(II), respectively. The Cu(II) complexes of L2 are six-coordinate [Cu(L2)2(NO3)2] (3) and [Cu(L2)2Cl(H2O)]Cl·H2O (4) species with distorted octahedral coordination geometries of the N4O2 and N2O3Cl donor atoms. A distorted octahedral coordination geometry of the N2O2Cl2 donor atoms is also found in the complex unit [Co(L2)2Cl2] of the Co(II) complex 5 but showing the oxygen atoms of the chelating ligand as well as the chloride ions in a cis-position. Depending on the complex, water molecules and chloride anions are shown to act as stabilizing components of the crystal structure. The comparative structural investigation includes also known structures of the bromine-free ligand analogue 2-(hydroxymethyl)pyridine, illustrating the basic implication of the bromine substitution, mostly perceptible in the different modes of crystal packing.
- Hubrich, Michael,Peukert, Max,Seichter, Wilhelm,Weber, Edwin
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body text
p. 1854 - 1862
(2010/07/04)
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- Synthesis, biological evaluation and molecular modelling studies of methyleneimidazole substituted biaryls as inhibitors of human 17α-hydroxylase-17,20-lyase (CYP17). Part I: Heterocyclic modifications of the core structure
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Novel chemical entities were prepared via Suzuki and SN reaction as AC-ring substrate mimetics of CYP17. The synthesised compounds 1-31 were tested for activity using human CYP17 expressed in Escherichia coli. Promising compounds were tested for selectivity against hepatic CYP enzymes (3A4, 2D6, 1A2, 2C9, 2C19, 2B6). Two potent inhibitors (27, IC50 = 373 nM/28, IC50 = 953 nM) were further examined in rats regarding their effects on plasma testosterone levels and their pharmacokinetic properties. Compound 28 was similarly active as abiraterone and showed better pharmacokinetic properties (higher bioavailability, t1/2 9.5 h vs 1.6 h). Docking studies revealed two new binding modes different from the one of the substrates and steroidal inhibitors.
- Jagusch, Carsten,Negri, Matthias,Hille, Ulrike E.,Hu, Qingzhong,Bartels, Marc,Jahn-Hoffmann, Kerstin,Mendieta, Mariano A.E. Pinto-Bazurco,Rodenwaldt, Barbara,Mueller-Vieira, Ursula,Schmidt, Dirk,Lauterbach, Thomas,Recanatini, Maurizio,Cavalli, Andrea,Hartmann, Rolf W.
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p. 1992 - 2010
(2008/09/20)
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- METHOD OF PREPARING INHIBITORS OF PHOSPHODIESTERASE-4
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In one aspect, the present invention is directed to a one pot method of preparing intermediates of Formula V, which are useful in making inhibitors of phosphodiesterase-4: The present invention is also directed to a method of preparing phosphodiesterase inhibitors comprising the Formula
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- ANTIVIRAL AGENT
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The present invention provides an integrase inhibitor. The inventors have have found the following compound of formula (I) possessing an integrase inhibitory activity. (wherein, R C and R D taken together with the neighboring carbon atoms form a ring which may be a condensed ring, Y is hydroxy, mercapto or amino; Z is O, S or NH ; R A is a group shown by (wherein, C ring is N-containing aromatic heterocycle) or the like)
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- 1-biaryl-1,8-naphthyridin-4-one phosphodiesterase-4 inhibitors
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Compounds represented by Formula (I): or a pharmaceutically acceptable salt thereof, are phosphodiesterrase 4 inhibitors useful in the treatment of asthma and inflammation.
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- Triazolopyridines. 18.1 nucleophilic substitution reactions on triazolopyridines; a new route to 2,2'-Bipyridines
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The synthesis of some 5-, 6-, and 7-halogenotriazolopyridines is described and their reactions with nucleophiles. The formation or 7,7'-bitriazolopyridines provides a new synthesis of 2,2'-bipyridines.
- Jones, Gurnos,Pitman, Mark A.,Lunt, Edward,Lythgoe, David J.,Abarca, Belen,Ballesteros, Rafael,Elmasnaouy, Mostafa
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p. 8257 - 8268
(2007/10/03)
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