- Synthesis and antiviral properties of new derivatives of 2-(alkylsulfanyl)-6-[1-(2,6-difluorophenyl)cyclopropyl]-5-methylpyrimidin-4(3H)-one
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Based on 2-(2,6-difluorophenyl)acetonitrile a synthesis was performed of new bioisosteric prochiral analogs of anti-HIV-1 active derivatives of 2-alkoxy-6-benzylpyrimidin-4(3Н)-one that we had previously obtained. The study using infected and nonifected strains of cells MT-4 made it possible to find in all prepared compounds a high anti-HIV activity whereas the cytotoxicity of the substances depended strongly on the structure of the alkylsulfanyl fragment of the molecule.
- Novakov,Yablokov,Orlinson,Navrotskii,Kirillov,Vernigora,Babushkin,Kachala,Schols
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- Preparation method of arylcyclopropane compound
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The present invention discloses a method for preparing an arylcyclopropane compound, 1.0eq phenylacetonitrile and 1.1eq 1-bromo-2-chloroethane as the starting material, N, N- dimethylacetamide as a solvent, solvent dosage of 10V, plus 2.5eq sodium hydride
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Paragraph 0089-0093; 0109-0113
(2022/01/10)
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- 1,3-SUBSTITUED PYRAZOLE COMPOUNDS USEFUL FOR REDUCTION OF VERY LONG CHAIN FATTY ACIC LEVELS
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Disclosed are chemical entities which are compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein Formula (I) has the structure: R1a, R1b, R2, R3, R4a, R4b and Y are as defined herein. These chemical entities are useful for reduction of very long chain fatty acid levels. These chemical entities and pharmaceutically acceptable compositions comprising such chemical entities can be useful for treating various diseases, disorders and conditions, such as adrenoleukodystrophy (ALD).
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Paragraph 326; 329
(2018/06/30)
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- Synthesis of 3-oxoesters and functional derivatives of pyrimidin-4(3Н)-one based on 1-(2,6-dihalophenyl)cyclopropan-1-carboxylic acids
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Special features of the synthesis and chemical transformations of novel functional derivatives of 6-[1-(2,6-dihalophenyl)cyclopropyl]pyrimidin-4(3H)-one and ethyl esters of 3-[1-(2,6-dihalophenyl)cyclopropyl]-2-methyl-3-oxopropanoic acids prepared from 2-(2,6-dihalophenyl)acetonitriles have been revealed. Novel achiral structural analogs of experimental anti-HIV agent МС-1501 have been synthesized.
- Novakov,Yablokov,Navrotskii,Mkrtchyan,Vernigora,Babushkin,Kachala,Ruchko
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p. 224 - 230
(2017/04/13)
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- Pd(II)-catalyzed enantioselective C-H activation of cyclopropanes
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Systematic ligand development has led to the identification of novel mono-N-protected amino acid ligands for Pd(II)-catalyzed enantioselective C-H activation of cyclopropanes. A diverse range of organoboron reagents can be used as coupling partners, and the reaction proceeds under mild conditions. These results provide a new retrosynthetic disconnection for the construction of enantioenriched cis-substituted cyclopropanecarboxylic acids.
- Wasa, Masayuki,Engle, Keary M.,Lin, David W.,Yoo, Eun Jeong,Yu, Jin-Quan
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p. 19598 - 19601
(2012/01/17)
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- Ortho-substituted benzyl esters of cyclopropanecarboxylic acids
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Ortho-substituted benzyl esters of cyclopropanecarboxylic acids I STR1 where X is N or CH and A is one of the following cyclopropane radicals: STR2 where R1 is CN, C2 -C8 -alkyl, CF3, C3 -C8 -alkenyl, (C1 -C4 -alkoxycarbonyl, unsubstituted or substituted phenyl-C1 -C6 -alkyl or phenyl-C3 -C6 -alkenyl, ethoxyphenyl, 2- or 3-bromophenyl, 2- or 4-trifluoromethylphenyl, 2,4- or 2,6-difluorophenyl, 2-fluoro-6-chlorophenyl, 2,4- or 2,6-dimethylphenyl, 2,3,6-trichlorophenyl or trimethylsilyl, R2 is H or halogen, R3 is unsubstituted or substituted phenyl, R4 is CH3 or halogen and Hal is halogen, with the proviso that X is CH when R1 is CF3 or trimethylsilyl, are suitable as fungicides and for controlling pests.
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