19838-08-5Relevant academic research and scientific papers
Preparation method of 2 (2-ethoxy-2-oxoethyl)-8-methyl-5, 6-dihydroimidazo pyrazine carboxylic acid tert-butyl ester
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Paragraph 0007; 0012; 0013, (2017/11/18)
The invention relates to a synthesizing method of 2 (2-ethoxy-2-oxoethyl)-8-methyl-5, 6-dihydroimidazo [1, 2-a] pyrazine-7 (8H)-carboxylic acid tert-butyl ester, and aims at solving the technical problem that a proper industrial synthesizing method is not provided currently. The method comprises the following four steps: 1, reacting a compound 1 and ammonium hydroxide in a high-pressure kettle to obtain a compound 2; 2, reacting the compound 2 and 4-epoxide-2-ethyl crotonate through acetonitrile to obtain a compound 3; 3, hydrogenating the compound 3 through a catalyst which is palladium/carbon in methanol to obtain a compound 4; and 4, adding Boc anhydride and potassium carbonate to the compound 4 in ethyl alcohol; and reacting overnight at room temperature to obtain a final compound 5.
PYRAZOLOPYRIMIDINES AS PROTEIN KINASE INHIBITORS
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Page/Page column 62, (2010/08/08)
The present invention relates to pyrazolopyrimidines of formula (I) wherein the substituents are as defined in the specification, to their use as pharmaceuticals, particularly for the treatment of hyperproliferative diseases and angiogenesis related disea
4- [HETEROCYCLYL-METHYL] -8-FLUORO-QUINOLIN-2-ONES USEFUL AS NITRIC OXIDE SYNTHASE INHIBITORS
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Page/Page column 67, (2009/04/25)
Novel compounds of formulae (II, III) and pharmaceutical compositions have been found to inhibit inducible NOS synthase wherein: R4, R5, R6 and R7 are independently selected from the group consisting of hydrogen, lower alkyl, and halogen; and, R8 has the structure whrein X1, X2, X3, X4, X5, X6, R9, R13, R14 and n are as described herein.
NOVEL SUBSTITUTED IMIDAZOLE DERIVATIVES
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Page/Page column 60, (2010/11/27)
The present invention relates to a compound represented by Formula [I] or a pharmaceutically acceptable salt or ester thereof: wherein: X1, X2, X3, and X4, which may be identical or different, are each C or N, provided that none to two of X1, X2, X3, and X4 is/are N; Y is CH or N; R1, R1', R2, R2', R3, R3', R4, and R4', which may be identical or different, are each a hydrogen atom, a lower alkyl group, or the like; R5 is a hydrogen atom or a methyl group; R6 and R7, which may be identical or different, are each a hydrogen atom, a lower alkyl group, or the like; R8 and R8', which may be identical or different, are each a hydrogen atom, a lower alkyl group, or the like; R9 is an aryl group or a heteroaryl group which may be substituted; and n is an integer from 1 to 3, and a PLK1 inhibitor or an anticancer agent containing the same.
ANGIOGENESIS INHIBITORS
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Page/Page column 17, (2008/06/13)
The present invention relates to the use of compounds for the treatment of angiogenesis related disorders involving a protein kinase as a medicament. The compounds e.g. have the general formula I. In preferred embodiments Rl and R5 are independently selec
PROTEIN KINASE INHIBITORS
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Page/Page column 15; 16, (2008/06/13)
The present invention relates to the use of compounds for the treatment of disorders involving a protein kinase, preferably a tyrosine kinase. The compounds e.g. have the general formula (I) wherein R1, R2 and R4 are indep
N-heterocyclyl sulphonamide derivatives and their use as endothelin antagonists
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, (2008/06/13)
The invention concerns pharmaceutically useful N-heterocyclyl sulphonamide derivatives, their pharmaceutically acceptable salts, processes for their manufacture, their use for antagonising one or more actions of endothelin in a human or other warm-blooded animal, their use in methods of treatment of diseases or medical conditions in which elevated or abnormal levels of endothelin play a significant causative role.
Studies on pyrazines; part 30: Synthesis of aminopyrazines from azidopyrazines
Sato,Matsuura,Miwa
, p. 931 - 934 (2007/10/02)
Azidopyrazines do not undergo reduction by reagents that are effective for the preparation of alkyl- or arylamines from the azides because the heterocyclic azides exist in the bicyclic form of tetrazolo[1,5-a]pyrazines. Nevertheless, the conversion into aminopyrazines was achieved by hydrogenolysis in the presence of ammonium hydroxide and palladium-on-carbon or particularly by reduction with tin(II) chloride in methanolic hydrochloric acid, in 34-87% yields. To elucidate the successful progress of the reaction, the equilibrium of azide-atetrazole was examined by 1H NMR spectroscopy in various solvents.
Studies on Pyrazines. 6. A Facile Separation Method for a Mixture of the Isomeric 2-Amino-3,5, and 6-methylpyrazines
Sato, Nobuhiro
, p. 143 - 147 (2007/10/02)
This paper describes a facile separation method for a mixture of the isomeric aminomethylpyrazines by two-stage processes.Thus the mixture of aminomethylpyrazines was converted into that of the aminobromomethylpyrazines, which could be separated by chromatography on silica gel.Each of the bromopyrazines was hydrogenated to regenerate the original aminopyrazine as a pure form.
