Chemical Name | (2R,3R,4S,5R)-2-(4-aminopyrrolo[1,2-f][1,2,4]triazin-7-yl)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-carbonitrile |
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Synonyms | (2R,3R,4S,5R)-2-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-carbonitrile; |
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CAS No. | 1191237-69-0 |
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Molecular Formula | C12H13N5O4 |
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Molecular Weight | 291.26300 |
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PSA | 149.92000 |
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LogP | -1.27552 |
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Preparation：
1) (3 r, 4 r, 5 r) - 2 - (4 - amino pyrrole and 4-trichlorobenzene [1] [2, 1 - f] triazine - 7 - base) - 4 - (benzyl oxygen) - 5 - (methyl benzyl oxygen radicals) - 3 - fluorine tetrahydrofuran - 2 - alcohol preparation, specific as follows: 3.4 G-7 bromopyrrole and [2, 1-F][1,2,4] -triazine-4-amine, 4.5mL trimethylchlorosilane (TMSCl) and 70mL tetrahydrofuran (THF) were added to the reaction bottle and stirred at room temperature for 2 hours. Then the reaction liquid was cooled to -78℃, adding 55mL, 1.0M n-butyllithium hexane solution (n-BuLi), stirring for 30 minutes, and then adding 70mLTHF solution containing 5.4g(3R, 4R, 5R)-4-(benzyloxy)-5-(benzyloxy methyl) -3-fluorodihydrofuran-2 (3H) -ketone. After dropping and stirring the reaction for 30 minutes, 42mL acetic acid was added to quench the reaction. The reaction solution was concentrated, diluted with 500mL ethyl acetate and washed with 250mL saturated NaCl solution. The organic layer is dried by anhydrous MgSO4, filtered and condensed under reduced pressure. The viscous liquid obtained was separated by silica gel column chromatography to obtain 2.6g white solid product.
2) (2R, 3R, 4R, 5R)-2-(4-aminopyrrole and [2, 1-F][1,2,4] triazine-7-yl)-4-(benzyloxy)-5-(benzyloxy methyl) -3-fluorotetrahydrofuran-2-methyl nitrile is prepared, specifically as follows: Add 2g(3R, 4R, 5R)-2-(4-aminopyrrole [2, 1-f] to the reaction flask [1,2, 4] triazine-7-yl)-4-(benzyloxy)-5-(benzyloxy methyl) -3-fluorotetrahydrofuran-2-ol, 100mL dichloromethane, 3.4mL trimethylnitrile-silane (TMSCN), 2.79g trimethylsilyl trifluoromesylate (TMSOTf). Stir the solution at -20 ° C for 4 hours. After the reaction is completed, 50mL saturated NaHCO3 solution, 300mL ethyl acetate and 100mL water are added to the reaction solution. The organic layer was separated and washed with 100mL saturated NaCl solution, dried with MgSO4, filtered and concentrated under reduced pressure. The viscous liquid was separated by silica gel column chromatography to obtain 0.82g white solid.
3) (2R, 3R, 4R, 5R)-2-(4-aminopyrrole [2, 1-F][1,2,4] triazine-7-yl) -3-fluoro-4-hydroxy-5 -(hydroxymethyl) tetrahydrofuran-2-methyl nitrile is prepared as follows: Add 1.1g(2R, 3R, 4R, 5R)-2-(4-aminopyrrole and [2, 1-F][1,2,4] triazine-7-yl)-4-(benzyloxy)-5-(benzyloxy methyl) -3-fluorotetrahydrofuran-2-methyl nitrile and 120mL dichloromethane into the reaction flask, stir and cool to 0℃. 77mL1.0MBBr3 dichloromethane solution was added to the reaction solution and stirred for 2 hours. Then the reaction liquid was cooled to -78 ° C, 34mL triethylamine was added, followed by 200mL methanol, and the temperature was raised to room temperature.
The reaction solution was concentrated under pressure, 200mL saturated sodium bicarbonate solution and 200mL dichloromethane were added, the solution was extracted, and the organic phase was concentrated under pressure. The concentrated liquid was separated by silica gel column chromatography to obtain 0.34g white solid, the intermediate 2 Redesivir mother nucleus.
Uses:
GS-441524 is a small molecule, the scientific name riboside triphosphate competitive inhibitor, which shows strong antiviral activity against many RNA viruses. It can inhibit the replication of several different types of RNA viruses, such as zoonotic Severe Acute Respiratory syndrome (SARS) coronavirus, Middle East Respiratory syndrome virus, Ebola virus, Lassa fever virus, Junin virus, and respiratory syncytial virus, while having low cytotoxicity in a wide range of cell lines.
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Company Introduction
hebei yanxi chemical co., LTD who registered capital of 10 million yuan, nearly to $2 million, we have a pharmaceutical raw materials factory production of pharmaceutical raw materials, and a reagent r&d center, and we do research and development production of reagent tens of thousands of species. our aim is quality strives for the survival. Seek development by credit reputation. Our products have big price advantage in Europe South America and so on .and Our company also has the advantage of high quality in Africa. in the past two years our products has reached more than 30 countries in the world, Europe. South America. North America, southeast Asia, Africa, etc. We welcome all over the world with the best quality and lowest price friend common cooperation and common development!
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