📜[(2R,3R,4R,5R)-5-(2-Amino-6-Chloropurin-9-yl)-4-Fluoro-4-Methyl-3-(Phenylcarbamoyloxy)Oxolan-2-Yl]Methyl N-Phenylcarbamate 在 N,N-二异丙基乙胺,N-[(Dimethylamino)-3-Oxo-1H-1,2,3-Triazolo[4,5-B]Pyridin-1-Yl-Methylene]-N-Methylmethanaminium Hexafluorophosphate体系中,用 甲醇,二氯甲烷作为反应溶剂,反应 18.0H,获得 Isopropyl ((S)-(((2R,3R,4R,5R)-5-(2-Amino-6-(Methylamino)-9H-Purin-9-yl)-4-Fluoro-3-Hydroxy-4-Methyltetrahydrofuran-2-yl)Methoxy)(Phenoxy)Phosphoryl)-L-Alaninate 参考文献:[En] Stereoselective Manufacture Of Selected Purine Phosphoramidates[Fr] Production Stéréosélective De Phosphoramidates De Purine Sélectionnés 标题:[En] Stereoselective Manufacture Of Selected Purine Phosphoramidates[Fr] Production Stéréosélective De Phosphoramidates De Purine Sélectionnés 摘要:本发明提供了制造磷酰胺酰核苷化合物1或其药学上可接受的盐的立体选择性过程.
1: Shannon A, Fattorini V, Sama B, Selisko B, Feracci M, Falcou C, Gauffre P, El Kazzi P, Delpal A, Decroly E, Alvarez K, Eydoux C, Guillemot JC, Moussa A, Good SS, La Colla P, Lin K, Sommadossi JP, Zhu Y, Yan X, Shi H, Ferron F, Canard B. A dual mechanism of action of AT-527 against SARS-CoV-2 polymerase. Nat Commun. 2022 Feb 2;13(1):621. doi: 10.1038/s41467-022-28113-1. 2: Good SS, Westover J, Jung KH, Zhou XJ, Moussa A, La Colla P, Collu G, Canard B, Sommadossi JP. AT-527, a Double Prodrug of a Guanosine Nucleotide Analog, Is a Potent Inhibitor of SARS-CoV-2 In Vitro and a Promising Oral Antiviral for Treatment of COVID-19. Antimicrob Agents Chemother. 2021 Mar 18;65(4):e02479-20. doi: 10.1128/AAC.02479-20. 3: Good SS, Moussa A, Zhou XJ, Pietropaolo K, Sommadossi JP. Preclinical evaluation of AT-527, a novel guanosine nucleotide prodrug with potent, pan- genotypic activity against hepatitis C virus. PLoS One. 2020 Jan 8;15(1):e0227104. doi: 10.1371/journal.pone.0227104.