- METHOD FOR PRODUCING 6-AMINO-2H-1,4-BENZOXAZINE-3(4H)-ONE
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PROBLEM TO BE SOLVED: To provide an industrially advantageous production method for 6-amino-2H-1,4-benzoxazine-3(4H)-one. SOLUTION: A method for producing 6-amino-2H-1,4-benzoxazine-3(4H)-one includes contact reduction and cyclization of the following compound, using a catalyst containing one or more metal atom selected from the group consisting of iron, cobalt, nickel and copper (R1 is a C1-C6 alkyl group; R2, R3 and R4 are the same or different to denote a C1-C6 alkyl group, a halogen atom or H). SELECTED DRAWING: None COPYRIGHT: (C)2020,JPOandINPIT
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Paragraph 0019-0020; 0025; 0027
(2020/04/01)
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- NITROGEN-CONTAINING BIOPOLYMER-BASED CATALYSTS, THEIR PREPARATION AND USES IN HYDROGENATION PROCESSES, REDUCTIVE DEHALOGENATION AND OXIDATION
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The present invention relates to a process for the preparation of a nitrogen containing biopolymer-based catalyst by pyrolysis of a metal complex with a nitrogen-containing biopolymer and to the nitrogen containing biopolymer-based catalysts obtainable by this process. In particular, the invention relates to a nitrogen containing biopolymer-based catalyst comprising metal particles and at least one nitrogen containing carbon layer. The invention also relates to the use of a nitrogen containing biopolymer-based catalyst in a hydrogenation process, preferably in a process for hydrogenation of nitroarenes, nitriles or imines; in a reductive dehalogenation process of C-X bonds, wherein X is CI, Br or I, preferably in a process for dehalogenation of organohalides or in a process for deuterium labelling of arenes via dehalogenation of organohalides; or in an oxidation process. Further, the invention relates to a metal complex with the nitrogen containing biopolymer, wherein the metal is a transition metal selected from the group consisting of manganese, ruthenium, cobalt, rhodium, nickel, palladium and platinum, preferably cobalt or nickel, and wherein the nitrogen containing biopolymer is selected from chitosan, chitin and a polyamino acid, preferably chitosan or chitin.
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Page/Page column 31-32; 34-35
(2018/07/29)
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- METHOD OF PRODUCING 6-AMINO-2H-1,4-BENZOXAZINE-3(4H)-ONES
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PROBLEM TO BE SOLVED: To provide an industrially advantageous method of producing 6-amino-2H-1,4-benzoxazine-3(4H)-ones. SOLUTION: There is provided a method of producing a compound represented by formula (2) by catalytic reduction and cyclization of a compound represented by formula (1), where R1 is C1-C6 alkyl, and R2-R4 are C1-C6 alkyl, halogen or H. SELECTED DRAWING: None COPYRIGHT: (C)2018,JPOandINPIT
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Paragraph 0017; 0019
(2018/10/03)
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- Synthesis technology of 1,4-benzoxazinone compound
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The invention relates to a synthesis technology of benzoxazinone compounds represented by formula I. The technology is characterized in that a dichlorobenzene derivative represented by formula II reacts with ethanolamide represented by formula III in the presence of a catalyst and an inorganic alkali to obtain the compound of formula I. R in the formula I and the formula II is selected from hydrogen, an amino group, a nitro group, a C1-6 alkyl group, a C1-6 alkoxy group and a hydroxyl group. The technology is a one-pot reaction method, realizes one-step direct cyclization, and has the advantages of simple reaction conditions, convenience in treatment, safe and highly-effective process, and high yield.
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Paragraph 0025-0027; 0037-0046
(2018/03/26)
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- NOVEL FUSED PYRIDINE DERIVATIVES USEFUL AS FAK/AURORA KINASE INHIBITORS
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This invention relates to certain novel pyrimidine derivatives of the Formula (I). The invention also relates to process for the preparation of the compound of the formula (I), pharmaceutical agents or compositions containing the compound or a method of using the compound for the treatment of proliferative diseases, such as cancer.
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- Synthetic technology for preparing 1,4-benzoxazinone through microwave process
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The invention relates to a preparation method for a benzoxazine compound. The method comprises the following steps: adding the compound shown as formula II, methyl alcohol and catalyst into a reactor; reacting under the existence of catalyst and alkali; and performing post-processing after ending the reaction, thereby acquiring the compound shown as formula I. In the formula, R group is selected from hydrogen, amino, nitro, C1-C6 alkyl, C1-C6 alkoxy and hydroxy; alkyl is selected from methyl, ethyl and isopropyl; alkoxy is selected from methoxy group, ethyoxyl and isopropoxy. The method is low in cost of raw materials, is safe and reliable, is completed under normal temperature and normal pressure and is simple in process.
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Paragraph 0019; 0020; 0021; 0031; 0032; 0033-0048
(2018/01/12)
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- Biomass-Derived Catalysts for Selective Hydrogenation of Nitroarenes
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Development of catalytically active materials from biowaste represents an important aspect of sustainable chemical research. Three heterogeneous materials were synthesized from inexpensive biomass-based chitosan and abundant Co(OAc)2 using complexation followed by pyrolysis at various temperatures. These materials were applied in the catalytic hydrogenation of nitroarenes using molecular hydrogen. A variety of diversely functionalized nitroarenes including some pharmaceutically active compounds were converted into aromatic amines in high yields, with high selectivity, and with excellent functional group tolerance. This green protocol has also been implemented for the synthesis of a biologically important TRPC3 inhibitor.
- Sahoo, Basudev,Formenti, Dario,Topf, Christoph,Bachmann, Stephan,Scalone, Michelangelo,Junge, Kathrin,Beller, Matthias
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p. 3035 - 3039
(2017/08/18)
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- Mild and selective hydrogenation of nitro compounds using palladium nanoparticles supported on amino-functionalized mesocellular foam
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We present the utilization of a heterogeneous catalyst comprised of Pd nanoparticles supported on aminopropyl-functionalized siliceous mesocellular foam (Pd0-AmP-MCF) for the selective hydrogenation of aromatic, aliphatic, and heterocyclic nitro compounds to the corresponding amines. In general, the catalytic protocol exclusively affords the desired amine products in excellent yields within short reaction times with the reactions performed at room temperature under ambient pressure of H2. Moreover, the reported Pd nanocatalyst displayed excellent structural integrity for this transformation as it could be recycled multiple times without any observable loss of activity or leaching of metal. In addition, the Pd nanocatalyst could be easily integrated into a continuous-flow device and used for the hydrogenation of 4-nitroanisole on a 2.5 g scale, where the product p-anisidine was obtained in 95% yield within 2 h with a Pd content of less than 1 ppm.
- Verho, Oscar,Gustafson, Karl P. J.,Nagendiran, Anuja,Tai, Cheuk-Wai,B?ckvall, Jan-E.
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p. 3153 - 3159
(2015/02/03)
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- COMPOSITIONS, SYNTHESIS, AND METHODS OF UTILIZING ARYLPIPERAZINE DERIVATIVES
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The present invention provides arylpiperazine derivatives which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder and depression.
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Page/Page column 14
(2010/09/05)
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- Compositions, Synthesis, And Methods Of Using Piperazine Based Antipsychotic Agents
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The present invention provides novel piperazine derivatives which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder and depression.
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Page/Page column 16; 22
(2009/12/23)
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- Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same
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Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.
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Page/Page column 49
(2008/06/13)
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- Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same
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Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.
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Page/Page column 25
(2010/11/23)
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- Discovery of potent, orally available vanilloid receptor-1 antagonists. Structure-activity relationship of N-aryl cinnamides
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The vanilloid receptor-1 (TRPV1 or VR1) is a member of the transient receptor potential (TRP) family of ion channels and plays a role in regulating the function of sensory nerves. A growing body of evidence demonstrates the therapeutic potential of TRPV1 modulators, particularly in the management of pain. As a result of our screening efforts, we identified (E)-3-(4-tert- butylphenyl)-N-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)acrylamide (1), an antagonist that blocks the capsaicin-induced and pH-induced uptake of 45Ca2+ in TRPV1-expressing Chinese hamster ovary cells with IC50 values of 17 ± 5 and 150 ± 80 nM, respectively. In this report, we describe the synthesis and structure-activity relationship of a series of N-aryl cinnamides, the most potent of which (49a and 49b) exhibit good oral bioavailability in rats (Foral = 39% and 17%, respectively).
- Doherty, Elizabeth M.,Fotsch, Christopher,Bo, Yunxin,Chakrabarti, Partha P.,Chen, Ning,Gavva, Narender,Han, Nianhe,Kelly, Michael G.,Kincaid, John,Klionsky, Lana,Liu, Qingyian,Ognyanov, Vassil I.,Tamir, Rami,Wang, Xianghong,Zhu, Jiawang,Norman, Mark H.,Treanor, James J. S.
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- UREA DERIVATIVES AS ANTAGONISTS OF THE VANILLOID RECEPTOR (VR1)
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This invention relates to urea derivatives according to general formula I and salts thereof which are useful as active ingredients of pharmaceutical preparations. The urea derivatives of the present invention have an excellent activity as VR1 antagonists
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Page/Page column 35
(2008/06/13)
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- 6- OR 7-(2-IMINO-2-IMIDAZOLIDINE)-1,4-BENZOXAZINES AS ALPHA ADRENERGIC AGENTS
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Compounds having α adrenergic activity and useful for the treatment of glaucoma, renal and gastrointestinal disorders and vasoconstictors have the formula STR1 where R 1 is independently H, or lower alkyl or 1 to 6 carbons; R 2 is independently H, or lower alkyl of 1 to 6 carbons or the two R 2 symbols jointly represent a carbonyl oxygen; R 3 is H, lower alkyl of one to 6 carbons, O, OH and OR 7 where R 7 is lower alkyl of 1 to 6 carbons, or R 3 is COH or COR 8 where R 8 is lower alkyl of 1 to 6 carbons; R 4 and R 5 independently is H, Br, Cl, or lower alkyl of 1 to 6 carbons, lower alkenyl or lower alkynyl with the proviso that when the R 2 groups symbolize a carbonyl oxygen then R 4 and R 5 both cannot be hydrogen; R 6 is hydrogen, Br, Cl, or lower alkyl of 1 to 6 carbons, lower alkenyl or lower alkynyl, and the R 5 and the (2-imidazoline-2-yl)amino substituents are connected mutually exclusively to the 6 and 7 positions of the 1,4-benzoxazine nucleus.
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- Tetrahydrophthalimides and their herbicidal use
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A compound of the formula: STR1 wherein R1 is a hydrogen atom, a C1 -C5 alkyl group, a C3 -C4 alkenyl group, a C3 -C4 alkynyl group, a C1 -C4 haloalkyl group, a C3 -C4 haloalkenyl group, a C3 -C4 haloalkynyl group, a C1 -C2 alkoxy(C1 -C2)alkyl group or a C1 -C2 alkoxy(C1 -C2)alkoxy(C1 -C2)alkyl group, R2 and R3 are, the same or different, each a hydrogen atom, a halogen atom, a C1 -C3 alkyl group or a phenyl group, X is a hydrogen atom, a chlorine atom or a fluorine atom and n is an integer of 0 or 1, which is useful as a herbicide.
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- Synthesis and Anthelmintic Activity of Some New 6- and 7-Isothiocyanato-2H-1,4-benzoxa(thia)zin-3(4H)-ones and Benzoxa(thia)zin-3(4H)-thiones
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A series of 6- and 7-isothiocyanato-2H-1,4-benzoxa(thia)zin-3(4H)-ones (8a-n, 9a-c, 12a-i and 12l) and thiones (10a-h and 11a-c) has been prepared for anthelmintic testing.Some of these compounds possess a significant degree of activity against hookworm i
- Shridhar, D. R.,Rao, K. Srinivasa,Singh, A. N.,Rastogi, K.,Jain, M. L.,et al.
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p. 1263 - 1267
(2007/10/02)
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