- New synthetic equivalent of nitromalonaldehyde treatable in organic media
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β-Nitroenamines having a formyl group at the β-position behave as the synthetic equivalent of unstable nitromalonaldehyde, which is a useful synthon for syntheses of versatile nitro compounds. High solubility of the nitroenamines into general organic solv
- Nishiwaki, Nagatoshi,Ogihara, Takuma,Takami, Toshiko,Tamura, Mina,Ariga, Masahiro
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- Method for synthesizing mild 4-aminoisoxazole hydrochloride
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The invention discloses a mild synthesis method of 4-aminoisoxazole hydrochloride, which comprises the following steps: 1) dissolving isoxazole in a mixed solvent of acetic acid and acetic anhydride,adding ammonium nitrate in batches while controlling the temperature, 2) after the reaction is finished, pouring into ice water, extracting by using ethyl acetate, combining organic phases, and concentrating to obtain 4nitro isoxazole, and 3) adding ethanol, concentrated hydrochloric acid and 5% palladium on carbon into the 4-nitroisoxazole, heating and pressurizing to react completely, cooling to0-10 DEG C, filtering, and washing with ice ethanol to obtain the 4-aminoisoxazole hydrochloride. According to the method, the nitration reaction is carried out under mild conditions, the risk is small, the method is suitable for industrial production, and the yield is greatly increased.
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Paragraph 0005; 0018-0023
(2021/03/10)
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- On the intrinsic reactivity of highly potent trypanocidal cruzain inhibitors
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The cysteine protease cruzipain is considered to be a validated target for therapeutic intervention in the treatment of Chagas disease. Hence, peptidomimetic cruzipain inhibitors having a reactive group (known as warhead) are subject to continuous studies
- Batista, Pedro Henrique Jatai,Bonatto, Vinicius,Cedron, Rodrigo,Cianni, Lorenzo,De Vita, Daniela,Franco, Caio Haddad,Montanari, Carlos A.,Moraes, Carolina Borsoi,Silva, Daniel G.,Tezuka, Daiane Y.,De Albuquerque, Sérgio,Lameira, Jer?nimo,Leit?o, Andrei
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supporting information
p. 1275 - 1284
(2020/12/01)
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- NOVEL COMPOUNDS
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The present invention discloses novel compounds inhibiting LRRK2 kinase activity, the preparation processes thereof, the compositions containing them, as well as the use in treating diseases characterized by LRRK2 kinase activity, particularly Parkinson's disease and Alzheimer's disease.
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Page/Page column 76
(2011/04/25)
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- SUBSTITUTED PYRIDAZINE CARBOXAMIDE COMPOUNDS AS KINASE INHIBITOR COMPOUNDS
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Pyridazine derivatives have unexpected drug properties as inhibitors of protein kinases and are useful in treating disorders related to abnormal protein kinase activities such as cancer.
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Page/Page column 37-38
(2010/01/12)
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- 65. Herstellung von substituierten 2-Aminooxazol-4-carbonitrilen.
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During our synthetic programme to convert 4-isoxazolylthioureas 3 into the corresponding carbodiimides 5, a side reaction leading to the hitherto unknown 2-aminooxazole-4-carbonitriles 6 was observed.By selecting appropriate reaction conditions, it was po
- Pascual, Alfons
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p. 556 - 569
(2007/10/02)
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- Synthesis of 4(5)-Acyl-, 1-Substituted 5-Acyl, and 1-Substituted 4-Acyl-1H-imidazoles from 4-Aminoisoxazoles
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4-Aminoisoxazoles can be acylated with a wide variety of activated carboxylic acids.Hydrogenation of the resulting amides gives α-(acylamino)enaminones, which cyclize to 4(5)-acylimidazoles upon treatment with base.This method allows for the synthesis of acylimidazoles with a wide range of substituents at C-2.Utilization of N-substituted 4-aminoisoxazoles in the same sequence of reactions yields 1-substituted 5-acylimidazoles, a substitution pattern not otherwise easily prepared.Treatment of α-(acylamino)enaminones, derived from N-unsubstituted isoxazoles, with primary amines leads to incorporation of the amine at the β-position with concomitant expulsion of ammonia.This sequence efficiently yields 1-substituted and 1,2-disubstituted 4-acylimidazoles but does not give satisfactory yields of 5-substituted 4-acylimidazoles due to steric inhibition of the amine exchange.
- Reiter, Lawrence A.
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p. 2714 - 2726
(2007/10/02)
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