- Preparation methods of 2,4-diamido-5-nitroso-6-hydroxypyridine and guanine
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The invention discloses a preparation method of 2,4-diamido-5-nitroso-6-hydroxypyridine. The preparation method comprises the following steps: (1) in a sodium methoxide methanol solution, carrying outa ring-closure reaction between methyl cyanoacetate and guanidine salt; (2) adding recycled absolute methanol to be diluted, filtering and recycling byproduct sodium nitrate; (3) concentrating a filter liquor, and recycling absolute methanol; (4) adding water to destroy excessive sodium methoxide, concentrating and recycling water-containing methyl alcohol; (5) in a diluted methane acid solution,carrying out a nitrosation reaction among an obtained concentrate, sodium nitrite and a nitrosation mother liquor; (6) after the reaction ends, carrying out cooling crystallization, filtering, takinga filter liquor as the nitrosation mother liquor to be used indiscriminately, and drying an obtained filter cake to obtain the 2,4-diamido-5-nitroso-6-hydroxypyridine. According to the preparation method, indiscriminate use of the nitrosation mother liquor and recycling of sodium nitrate and methyl alcohol are realized, and simultaneously the diluted methane acid solution is used for replacing concentrated sulfuric acid used, in the prior art, to carry out the nitrosation reaction, so that the recycling of a solvent and a reagent is facilitated, and the displacement of waste water is reduced.
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Paragraph 0058; 0059; 0060; 0061; 0067; 0068; 0069; 0070
(2018/10/19)
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- Synthesis and in vitro evaluation of 2-amino-4-N-piperazinyl-6-(3,4- dimethoxyphenyl)-pteridines as dual immunosuppressive and anti-inflammatory agents
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Screening of a pteridine-based compound library led to the identification of compounds exhibiting immunosuppressive as well as anti-inflammatory activity. Optimization afforded a series of 2-amino-4-N-piperazinyl-6-(3,4- dimethoxyphenyl)pteridine analogues. The most potent congeners in this series displayed low nM IC50 values in the Mixed Lymphocyte Reaction (MLR) assay. In addition, these compounds also have potent anti-inflammatory activity as measured in the Tumor Necrosis Factor (TNF) assay.
- De Jonghe, Steven,Marchand, Arnaud,Gao, Ling-Jie,Calleja, Agnes,Cuveliers, Eva,Sienaert, Ilse,Herman, Jean,Clydesdale, Gavin,Sefrioui, Hassane,Lin, Yuan,Pfleiderer, Wolfgang,Waer, Mark,Herdewijn, Piet
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scheme or table
p. 145 - 149
(2011/02/25)
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- Immunosuppressive effects of pteridine derivatives
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This invention relates to a group of trisubstituted and tetrasubstituted pteridine derivatives, their pharmaceutically acceptable salts, N-oxides, solvates, dihydro- and tetrahydroderivatives and enantiomers, possessing unexpectedly desirable pharmaceutical properties, in particular which are highly active immunosuppressive agents, and as such are useful in the treatment in transplant rejection and/or in the treatment of certain inflammatory diseases. These compounds are also useful in preventing or treating cardiovascular disorders, allergic conditions, disorders of the central nervous system and cell proliferative disorders.
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