- Preparation method of 2-chloro-4-aminopyridine
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The invention belongs to the field of organic synthesis, and particularly relates to a preparation method of 2-chloro-4-aminopyridine. The preparation method comprises the following steps: (1) using 2-chloropyridine as a raw material and chloroform as a solvent, and generating 2-chloropyridine oxide under the action of m-chloroperoxybenzoic acid; (2) reacting 2-chloropyridine oxide with a mixed acid composed of concentrated nitric acid and concentrated sulfuric acid to generate 2-chloro-4-nitropyridine oxynitride; and (3) reducing 2-chloro-4-nitropyridine oxynitride into 2-chloro-4-aminopyridine. The method has the beneficial effects that the reaction conditions are mild, the operation is easy, the post-treatment is simple, the scale-up production is easy, the method is very suitable for industrial production; the catalytic effect is good, the yield is high; the raw materials are cheap, and the production cost is low.
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Paragraph 0016; 0019; 0021; 0023; 0025; 0028; 0029
(2020/05/05)
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- A 2 - chloro -4 - aminopyridine preparation method
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The invention belongs to the field of organic synthesis, in particular relates to a 2 - chloro - 4 - aminopyridine preparation method, comprises the following steps: (1) to 2 - chloro pyridine as raw materials, chloroform as solvent, under the action of the meta-chloroperoxybenzoic acid to produce 2 - chloro pyridine oxide; (2) 2 - chloro pyridine oxide by the concentrated nitric acid in concentrated sulfuric acid the acid produced by the reaction of a 2 - chloro - 4 - nitro pyridine nitrogen oxides; (3) 2 - chloro - 4 - nitro pyridine nitrogen oxide reduction is 2 - chloro - 4 - aminopyridine. 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; good catalytic effect, high yield; low prices of raw materials, the production cost is low.
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Paragraph 0016; 0019; 0021; 0023; 0025; 0028; 0030
(2019/05/28)
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- Design and synthesis of purine analogues as highly specific ligands for FcyB, a ubiquitous fungal nucleobase transporter
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In the course of our study on fungal purine transporters, a number of new 3-deazapurine analogues have been rationally designed, based on the interaction of purine substrates with the Aspergillus nidulans FcyB carrier, and synthesized following an effective synthetic procedure. Certain derivatives have been found to specifically inhibit FcyB-mediated [3H]-adenine uptake. Molecular simulations have been performed, suggesting that all active compounds interact with FcyB through the formation of hydrogen bonds with Asn163, while the insertion of hydrophobic fragments at position 9 and N6 of 3-deazaadenine enhanced the inhibition.
- Lougiakis, Nikolaos,Gavriil, Efthymios-Spyridon,Kairis, Markelos,Sioupouli, Georgia,Lambrinidis, George,Benaki, Dimitra,Krypotou, Emilia,Mikros, Emmanuel,Marakos, Panagiotis,Pouli, Nicole,Diallinas, George
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p. 5941 - 5952
(2016/11/09)
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- 9H-PYRROLO-DIPYRIDINE DERIVATIVES
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The invention relates to 9H-pyrrolo-dipyridine derivatives of formula I, processes for preparing them, pharmaceutical compositions containing them and their use as radiopharmaceuticals in particular as imaging agents for the detection of Tau aggregates.
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Page/Page column 66
(2016/09/22)
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- NOVEL 6-ARYLAMINO PYRIDONE SULFONAMIDES AND 6-ARYLAMINO PYRAZINONE SULFONAMIDES AS MEK INHIBITORS
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The invention provides novel substituted 6-arylamino pyridone sulfonamides and 6 arylamino pyrazinone sulfonamides represented by Formula I, or a pharmaceutically acceptable salt, solvate, polymorph, ester, tautomer or prodrug thereof, and a composition comprising these compounds. The compounds provided can be used as inhibitors of MEK and are useful in the treatment of inflammatory diseases, cancer and other hyperproliferative diseases. The invention further provides a method of treatment for inflammatory diseases, cancer and other hyperproliferative diseases in mammals, especially humans
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Page/Page column 79-80
(2010/12/31)
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- Keratin dyeing compounds, keratin dyeing compositions containing them, and use thereof
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Compositions for the oxidative dyeing of keratin fibers, comprising a medium suitable for dyeing and at least one N-oxides of six-membered rings with one or two nitrogen atoms keratin dyeing compound. A method for oxidative dyeing of keratin fibers, comprising applying such compositions in the presence of an oxidizing agent, for a period sufficient to develop the desired coloration.
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Page/Page column 9
(2008/06/13)
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- N-(unsubstituted or substituted)-4-substituted-6-(unsubstituted or substituted)phenoxy-2-pyridinecarboxamides or thiocarboxamides, processes for producing the same, and herbicides
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N-(substituted or unsubstituted)-4-substituted-6-(substituted or unsubstituted) phenoxy-2-pyridine carboxamide or thiocarboxamide represented by the general formula (I) and a process for producing the compound. A herbicide containing as an effective ingredient N-(substituted or unsubstituted)-4-substituted-6-(substituted or unsubstituted) phenoxy-2-pyridine carboxamide or thiocarboxamide represented by the general formula (I).
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Referential example 2
(2010/01/30)
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- Vitronectin receptor antagonists
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Compounds of the formula (I) are disclosed which are vitronectin receptor antagonists and are useful in the treatment of osteoporosis: or a pharmaceutically acceptable salt thereof.
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- 6-(Nonsubstituted or substituted) phenoxy picolinic acids, process of preparing the same, and agricultural/horticultural germicides containing the same
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An agricultural or horticultural fungicide containing 6-(unsubstituted or substituted) phenoxy picolinic acid represented by the general formula (I), as an effective ingredient. wherein R is a halogen atom, a C1to C4alkyl group, a C1to C4haloalkyl group, a C1to C4alkoxy group, a C1to C4haloalkoxy group, a C1to C4alkylthio group, a C1to C4alkylamino group, a di(C1to C4alkyl)amino group or a C7to C8aralkyl(C1to C4alkyl)amino group; n2is an integer of 0 to 3; Y is a C1to C4alkyl group, a C1to C4haloalkyl group, a C1to C4alkoxy group, a C1to C4haloalkoxy group, a C1to C4alkylthio group, a C1to C4haloalkylthio group or a halogen atom; and m is an integer of 0 to 5, and when m and n2are not less than 2, Rs and Ys may be the same or different, respectively. The compound is useful as an effective ingredient of agricultural or horticultural fungicides.
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- 6-phenoxy picolinic acid alkylidene hydrazide derivative, process for producing the same and herbicide using the same
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PCT No. PCT/JP98/02842 Sec. 371 Date Feb. 23, 2000 Sec. 102(e) Date Feb. 23, 2000 PCT Filed Jun. 25, 1998 PCT Pub. No. WO99/00370 PCT Pub. Date Jan. 7, 1999A 6-phenoxy picolinic acid alkylidene hydrazide derivative, a process for producing the derivative and a herbicide containing the derivative as an effective ingredient. Such a compound is a novel compound and is useful as an effective ingredient of herbicides.
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- Synthesis of the analogue nucleoside 3-deaza-2'-deoxycytidine and its template activity with DNA polymerase
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A new synthesis of the nucleoside analogue 3-deaza-2'-deoxycytidine is described. The N3-nitrogen of dC is involved in the central hydrogen bond of a dG-dC base pair. The relative importance of hydrogen bonding as a controlling factor in the activity of DNA polymerase is examined by studying both duplex stability and template effects for this dc3C nucleoside. Duplexes containing dG-dc3C base pairs were strongly destabilized while templates containing the analogue nucleoside were found to incorporate only the complementary dG triphosphate, similar to observations with templates containing the native 2'-deoxycytidine.
- Searls, Tim,McLaughlin, Larry W.
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p. 11985 - 11996
(2007/10/03)
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- Structural and vibrational investigation of 2-amino-4-nitropyridine crystal
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The X-ray structure of 2-amino-4-nitropyridine was determined at room temperature. The crystal belongs to the P2(I)/c space group of the monoclinic system (Z = 4, a = 6.7290(10), b = 10.946(2), c = 9.060(2) A, β = 100.03(3) deg) and is built of layers parallel to the (102) crystallographic plane. The molecules in the layer are joined into centrosymmetric dimers by two N-H···N hydrogen bonds (N···N distance = 3.011(3) A), which form rings of C(i) symmetry. The other N-H bonds of the amino groups are involved in N-H···O hydrogen bonds with the oxygen atoms of the nitro groups (N···O distance = 3.054(3) A). These hydrogen bonds join the dimers into an infinite plane. The powder IR and Raman spectra (4000-80 cm-1) were measured for normal and deuterated crystals and are discussed with respect to the crystal structure. The N-H stretching vibrations behave as the stretching vibrations of two almost independent hydrogen bonds. Strong A(g)-A(u)-type splitting is observed for the stretching vibrations of the N-H···N type hydrogen bonds.
- Oszust,Talik,Pietraszko,Marchewka,Baran
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- Synthesis of 'A' Ring Isomazole Oxypropanolamines via Hydrolysis of 1H-Imidazopyridine Oxazolidin-2-ones
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The hydrolysis of oxazolidin-2-one 15, under forcing conditions, gives the oxypropanolamine 7 and 4,5-dihydro-1H-imidazopyridin-4-ones (17-19) and may occur by a BAL mechanism, involving intramolecular nucleophilic attack by pyridyl nitrogen.
- Barraclough, Paul,Gillam, Janet,King, W. Richard,Nebbs, Malcolm S.,Vine, Susan J.
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p. 1359 - 1376
(2007/10/03)
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- Periselectivity between the and Thermal Sigmatropic Rearrangements of 2-Allyloxypyridine N-Oxides
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Thermal rearrangement of 2-allyloxypyridine N-oxides (4a-c) yields N-allyloxy-2-pyridones (5a-c) and 3-allyl-N-hydroxy-2-pyridones (6a-c).These transformations are shown to be regiospecific and on this basis it is proposed that the reactions involve concerted and sigmatropic rearrangements.Supporting evidence based on solvent effects, temperature effects, and substituent effects is given.
- Alker, David,Ollis, W. David,Shahriari-Zavareh, Hooshang
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p. 1623 - 1630
(2007/10/02)
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- Pyridinylurea N-oxide compounds and agricultural uses
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Pyridinylurea N-oxides of the formula STR1 and acid addition salts thereof; wherein R is cycloalkyl (C3 -C8), alkenyl (C3 -C8), or an alkyl (C1 -C6) group optionally substituted with halogen, hydroxy, cycloalkyl (C3 -C8) alkoxy (C1 -C6), dialkyl (C1 -C6)amino or phenyl; R1 is hydrogen or alkyl (C1 -C6); R and R1 together with the nitrogen atom of the NRR1 group optionally define a nonaromatic heterocycle containing 4 to 6 ring carbon atoms; each X independently is halogen, alkyl (C1 -C6), haloalkyl (C1 -C6), alkoxy (C1 -C6), hydroxy, 2-pyridinyl, alkyl(C1 -C6)thio or alkyl (C1 -C6)sulfonyl; A is 1 to 4; and wherein the NHCONRR1 group is bonded to the pyridinyl ring in the 3- or 4-position. The compounds are useful in agriculture as plant growth regulators.
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- Pharmaceutical compositions
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Compounds which are a 1-hydroxypyrid-2-one in which one or more of the hydrogen atoms attached to ring carbon atoms are replaced by a substituent selected from aliphatic acyl, aliphatic amide, aliphatic amine, carboxy, cyano, aliphatic ester, halogen, hydroxy and sulpho groups, alkoxy groups and alkoxy groups substituted by an alkoxy, aliphatic amide, aliphatic amine, aliphatic ester, halogen or hydroxy group, aliphatic hydrocarbon groups and aliphatic hydrocarbon groups substituted by an alkoxy, aliphatic ester, halogen or hydroxy group, but excluding compounds in which said replacement of hydrogen atoms in the compound is effected only by substituents selected from aliphatic hydrocarbon groups, halogen groups and aliphatic hydrocarbon groups substituted by a halogen group, or a salt thereof containing a physiolgically acceptable ion or ions, are of value in the treatment of patients having a toxic concentration of a metal, particularly iron, in the body whilst the iron complexes of such compounds are of value in the treatment of iron deficiency anaemia.
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