- Probes for imidazoline binding sites: Synthesis and evaluation of a selective, irreversible I2 ligand
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An irreversible ligand (7) has been prepared based on the selective I2 ligand 2-BFI. Compound 7 displayed high affinity and selectivity for I2-sites and has been shown to irreversibly bind to these sites in rat brain. Compound 7 should, therefore, prove an invaluable tool for the further elucidation of I2-site function. (C) 2000 Elsevier Science Ltd. All rights reserved.
- Coates, Philippa A.,Grundt, Peter,Robinson, Emma S.J.,Nutt, David J.,Tyacke, Robin,Hudson, Alan L.,Lewis, John W.,Husbands, Stephen M.
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Read Online
- Method for preparing benzofuran-2-carboxamide compound
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The invention discloses a method for preparing a benzofuran-2-carboxamide compound. The method comprises the following steps: sequentially adding an alkali and a 2-formylaryloxy acetonitrile derivative into a solvent, and carrying out a reaction at a certain temperature to obtain a reaction solution after complete reaction; and sequentially subjecting the reaction solution to extraction, drying, concentration and column chromatographic separation to obtain a target product, i.e., the benzofuran-2-carboxamide compound. According to the invention, common cheap easily-available inorganic base ororganic base is used as a catalyst of the reaction, no metal or organic catalyst is used, and no additive is needed; reaction conditions are mild; product yield is high; operation is simple; and the method is environment-friendly. Reagents and the catalyst used in the method are rich in industrial sources and easy to obtain, so production cost is low; product purity is high; and the method has good industrial application prospects.
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Paragraph 0024-0028
(2020/01/25)
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- Pyrimidine heterocyclic compounds, pyrimidine heterocyclic compound salts, and preparation method and application thereof
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The invention provides pyrimidine heterocyclic compounds, pyrimidine heterocyclic compound salts, and a preparation method and application thereof. According to the pyrimidine heterocyclic compounds provided by the invention, specific Rq is selected, so that the obtained compounds have favorable drug resistance and long half life when being used as the medicine for treating or preventing HIV. The compounds have the advantages of high activity, low toxicity and high stability.
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Paragraph 0147; 0154; 0155; 0156
(2017/07/26)
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- POLYMORPHIC FORM OF 5-(4-[4-(5-CYANO-1H-INDOL-3-YL) BUTYL] PIPERAZIN-1-YL) BENZOFURAN-2-CARBOXAMIDE AND PROCESS FOR PREPARING THEREOF
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The present invention provides a solid state Form-Z of 5-(4-[4-(5-cyano-1H-indol-3-yl)butyl]piperazin-1-yl)benzofuran-2-carboxamide. The present invention also provides a process for preparing Form-Z of 5-(4-[4-(5-cyano-1H-indol-3-yl)butyl]piperazin-1-yl)benzofuran-2-carboxamide comprising the steps of i) reacting solid state form of 5-(1-piperazinyl)benzofuran-2-carboxamide or its salts with 3-(4-chlorobutyl)-1H-indole-5-carbonitrile an organic solvent in presence of a base to obtain crude vilazodone free base; ii) purifying the crude vilazodone free base of step (i) in an organic solvent; iii) treating the purified vilazodone free base of step (ii) with an organic solvent to obtain solid state form-Z of vilazodone. The present invention further provides a pharmaceutical composition comprising a therapeutically effective amount of an amorphous form of vilazodone hydrochloride and use of solid state Form-Z of vilazodone for the treatment of major depressive disorders.
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Paragraph 0083
(2014/07/08)
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- PROCESS FOR THE PREPARATION OF VILAZODONE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF
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The present invention provides a novel intermediate of vilazodone and its process of preparation. The present invention further provides a process for preparing vilazodone or a pharmaceutically acceptable salt thereof using said novel intermediate.
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Page/Page column 14; 15
(2014/05/07)
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- POLYMORPHIC FORM OF 5-(4-[4-(5-CYANO-1H-INDOL-3- YL)BUTYL]PIPERAZIN-1-YL) BENZOFURAN-2-CARBOXAMIDE
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The present invention relates to a process for the preparation of 5-(4-[4-(5- cyano- 1 H-indol-3 -yl)butyl] piperazin- 1 -yl)benzofuran-2-carboxamide of Formula (1) or its pharmaceutically acceptable salt, solvates or hydrates thereof. In particular, the present invention provides a novel intermediate compound, 5-(4-substitutedpiperazin- 1-yl)benzofuran-2-carboxamide of Formula (X). The present invention further provides solid state form of 5-(4-[4-(5-cyano-1H-indol-3- yl) butyl]piperazin-1-yl)benzofuran-2-carboxamide of Formula (1) and process for its preparation.
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Page/Page column 22
(2014/01/07)
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