- Preparation method of dichloro dialkyl fumaronitrile
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The preparation method comprises the following steps: I raw materials are taken as raw materials, and chlorine or N - chlorosuccinimide is used as a chlorination reagent for chlorination reaction to generate compound II. The condensation reaction of compound II with cyanoacetamide is carried out under the action of a base to give compound III. The compound III is chlororeacted with phosphorus oxychloride to give a dichloro dialkyl nicotinonitrile. The preparation method avoids the use of sulfonyl chloride as a chlorination reagent, thereby avoiding the generation of sulfur dioxide tail gas, and preventing the generated acid waste gas from corroding equipment and the like.
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- Route Of Synthesis For Opicapone
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The present invention relates to a new route of synthesis for obtaining Opicapone ((4Z)-4-[3-(2,5-dichloro-4,6-dimethyl-1-oxidopyridin-1-ium-3-yl)-2H-1,2,4-oxadia-zol-5-ylidene]-2-hydroxy-6-nitrocyclohexa-2,5-dien-1-one), new intermediates in the reaction path and the new substance 2,5-dichloro-N-hydroxy-4,6-dimethylpyridine-3-carboximidoyl chloride.
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Paragraph 0042; 0043; 0044
(2019/01/10)
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- A structure-activity relationship study of the positive allosteric modulator LY2033298 at the M4 muscarinic acetylcholine receptor
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Positive allosteric modulators (PAMs) targeting the M4 muscarinic acetylcholine receptor (mAChR) offer greater sub-type selectivity and unique potential as central nervous system agents through their novel mode of action to traditional orthosteric ligands. In an attempt to elucidate the molecular determinants of allostery mediated by the exemplar thienopyridine M4 mAChR PAM, LY2033298, we report herein a systematic structure-activity relationship (SAR) study investigating different linkage points, halogen replacements to examine size and electronic effects, and different substitution combinations on the thienopyridine scaffold. We applied an operational model of allosterism to determine values of functional affinity (KB), cooperativity (αβ) and intrinsic agonism (τB) for all compounds.
- Szabo, Monika,Huynh, Tracey,Valant, Celine,Lane, J. Robert,Sexton, Patrick M.,Christopoulos, Arthur,Capuano, Ben
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supporting information
p. 1998 - 2003
(2015/11/17)
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- CHEMICAL COMPOUND USEFUL AS INTERMEDIATE FOR PREPARING A CATECHOL-O-METHYLTRANSFERASE INHIBITOR
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There is disclosed a methylated intermediate which may be demethylated to provide an inhibitor of catechol-O-methyltransferase useful in the treatment of Parkinson's disease. Also disclosed are methods of making and using said intermediate.
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Page/Page column 15-16
(2013/07/05)
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- Oxadiazole derivatives as COMT inhibitors
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This invention relates to novel substituted [1,2,4]-oxadiazoles, their use in the treatment of some central and peripheral nervous system disorders, methods for their preparation and pharmaceutical compositions containing them.
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Page/Page column 6-7
(2008/06/13)
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- Synthesis of some halogen- and nitro-substituted nicotinic acids and their fragmentation under electron impact
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Features of electrophilic and nucleophilic substitution under chlorination and nitration reactions conditions have been investigated for 6-hydroxy- and 6-methyl-substituted derivatives of 3-cyano-4-methyl-2(1H)-pyridones. The polychloro- and nitro-substituted 3-cyano-4-methylpyridines obtained were used as synthons in the synthesis of some polyhalo- and nitro-substituted nicotinic acids and their amides. The fragmentation pathways of the synthesized compounds under electron impact have been studied.
- Dyadyuchenko,Strelkov,Mikhailichenko,Zaplishny
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p. 308 - 314
(2007/10/03)
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