- NITRATION OF ACETYL DERIVATIVES OF 1-METHYLPYRAZOLE
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The nitration of acetyl-substituted 1-methylpyrazoles with nitric acid in 20percent oleum and in acetic anhydride was studied.Dipyrazolofuroxans are formed in the case of nitration in oleum. 4-Nitro-3-acetyl-1-methylpyrazole was obtained by nitration of 3-acetyl-1-methylpyrazole in acetic anhydride.
- Manaev, Yu. A.,Khrapov, A. V.,Perevalov, V. P.
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- CYCLIC SULFAMIDE COMPOUNDS AND METHODS OF USING SAME
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The present disclosure provides, in part, cyclic sulfamide compounds, and pharmaceutical compositions thereof, useful as modulators of Hepatitis B (HBV) core protein, and methods of treating Hepatitis B (HBV) infection.
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Page/Page column 176-177
(2018/09/21)
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- Pyrimidinone Derivatives as Antimalarial Agents
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The invention relates to novel pyrimidinone-based heterocyclic compounds which are parasite growth inhibitors, having the general formula (I) in which Y is a morpholine chosen from three bridged morpholines, L is a bond or a linker, n=0 or 1 and R2 is a methyl group when n=0 and a hydrogen atom when n=1. Process for the preparation thereof and therapeutic use thereof.
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Paragraph 0806; 0807; 0808; 0809
(2015/07/15)
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- 4,6-DIARYLAMINOTHIAZINES AS BACE1 INHIBITORS AND THEIR USE FOR THE REDUCTION OF BETA-AMYLOID PRODUCTION
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Compounds of formula (I), including pharmaceutically acceptable salts thereof, are set forth herein: (I) wherein R1 and R2 are independently hydrogen, or -CH3; or R1 and R2 can join together in a ring by adding -(CH2)4-; R3 is hydrogen or C1-C3 al-kyl; Y and Z are independently a C6-C10- aryl group or a 5-10 membered heterocyclic group which can be further substituted with from 0-3 substituents selected from the group of halogen, hydroxy, amino, C1-4 alkylamino, C1-4 dialkylamino, halo C1-4 alkyl, CN, C1-C6, alkyl or cycloalkyl, C1-C6 alkoxy, -C=OC1-4 alkyl, -SO2C1-4 alkyl, and C2-C4 alkynyl; A is selected from the group of phenyl, ben-zyl, oxazolyl, thiazolyl, isoxazolyl, imidazolyl, pyrazolyl, pyridyl, pyrimidinyl, and pyrazinyl groups which can be further substituted with from 0-3 substituents selected from the group of halogen, hydroxy, amino, C1-4 alkylamino, C1-4 dialkylamino, haloC1-4 alkyl, hydroxyC1-6 alkyl, CN, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, and C2-C4 alkynyl; L is -NHCO-, or is a single bond; and L and Z to-gether can be absent
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Page/Page column 72
(2014/07/08)
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- PYRIMIDINONE DERIVATIVES AS ANTIMALARIAL AGENTS
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The invention relates to novel pyrimidinone-based heterocyclic compounds which are parasite growth inhibitors, having the general formula (I) in which Y is a morpholine chosen from three bridged morpholines, L is a bond or a linker, n = 0 or 1 and R2 is a methyl group when n = 0 and a hydrogen atom when n = 1. Process for the preparation thereof and therapeutic use thereof.
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Page/Page column 48; 49; 88
(2014/01/09)
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- An efficient synthesis of isomeric 1-(1-Alkyl-1H-pyrazolyl) ethanones
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A simple and versatile general method for the preparation of N-substituted 3-, 4-, or 5-acetylpyrazoles from corresponding acids via hydrolysis and decarboxylation of substituted diethyl [(1-alkyl-1H-pyrazolyl)carbonyl]malonates was developed. Title compounds were prepared in three steps without isolation of intermediates in 48-82% overall yield.
- Taydakov, Ilya,Krasnoselskiy, Sergey
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p. 1422 - 1424
(2013/02/23)
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