D-核糖置于盐酸,乙酸酐,二甲基亚砜体系中,用 1,4-二氧六环,水,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 24.0H,反应生成 2,3,5-三苄氧基-D-核糖酸-1,4-内酯 参考文献:Synthesis Of C-Spiro-Glycoconjugates From Sugar Lactones Via Zinc Mediated Barbier Reaction 标题:Synthesis Of C-Spiro-Glycoconjugates From Sugar Lactones Via Zinc Mediated Barbier Reaction 摘要:使用zn粉和催化量的tmscl作为活化剂,在barbier反应条件下实现了糖1,5和1,4内酯的anomeric双二烯基化,单-β-罗汀基化和单-β-丙炔基化.合成的双二烯基衍生物经过环闭合烯烃复分解反应得到c-螺环戊烯糖苷.最后,将环戊烯环转化为基于碳水化合物的三环吗啉并三唑糖缀合物,作为潜在的sglt2抑制剂. DOI:10.1039/c3Ra46796A
专利号:WO-2023126968-A1 优先权日:2021-12-29 标 题 :A process for the synthesis of bcx-1777 and bcx-4430 发明人:LANKALAPALLI RAVI SHANKAR; KARUNAKARAN ANITHA KRISHNAKUMAR; SURESH SANJAY VARMA; VELICKAKATHU OMANAKUTTAN YADHUKRISHNAN; KAPIYA SANGEETH; VALAPPIL SHIHAS AHAMMED CHEKRAIN; BERNARD PRABHA; THANGARASU ARUN KUMAR; DODDRAMAPPA DODDAMANI SHRIDEVI; JOHN JUBI; KOKKUVAYIL VASU RADHAKRISHNAN; AYYAPPANPILLAI AJAYAGHOSH 权利人:COUNCIL SCIENT IND RES 摘要:The present invention is concerned with a novel convergent route for synthesis of BCX-1777 and BCX-4430. Two key starting materials that were carefully chosen for cross-coupling were a stable sugar intermediate, unlike the imine intermediates in the prior art, and dihalogenated pyrrolopyrimidine intermediate. A chemoselective cross-coupling was achieved from the two key starting materials, which upon reduction and activation resulted in stereoselective formation of an advanced intermediate in 55% yield from protected D-ribonolactone in 6 steps. The advanced intermediate then served as a starting material for synthesis of BCX-1777 and BCX-4430 in 38% (over 8 steps) and 32% (over 9 steps) yields, respectively from protected D-ribonolactone.
专利号:US-11612614-B2 优先权日:2020-10-20 标题:Isomorphs of Remdesivir and methods for synthesis of same 发明人:TRIPATHI VINAY SHANKAR; PATEL AKSHAY NIKHIL 权利人:ANZALP PHARMASOLUTIONS PVT LTD 摘要:A new isoform of 2-ethylbutyl (2S)-2-[[[(2R,3S,4R,5R)-5-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-5-cyano-3/4-dihydroxyoxolan-2-yl]methoxy-phenoxyphosphoryl]amino]propanoate (Remdesivir) having increased water solubility is disclosed, along with methods for making the same. Also disclosed are solid and liquid pharmaceutical compositions suitable for treating viral infections such as Arenaviridae, Coronaviridae, Filoviridae, Flaviviridae, or Paramyxoviridae viral infections which contain an effective amount of Remdesivir prepared according to the inventive method and the use of those compositions for treating such viral infections.
专利号:US-2021228605-A1 优先权日:2020-10-20 标题:Isomorphs of remdesivir and methods for synthesis of same
专利号:US-2021161927-A1 优先权日:2020-10-20 标 题:Isomorphs of remdesivir and methods for synthesis of same
专利号:US-9828388-B2 优先权日:2014-07-28 标题:Thieno[3,2-d]pyrimidine, furo[3,2-d]pyrimidine, and pyrrolo[3,2-D]pyrimidines useful for treating respiratory syncitial virus infections 发明人:CLARKE MICHAEL O'NEIL HANRAHAN; MACKMAN RICHARD L; SIEGEL DUSTIN 权利人:GILEAD SCIENCES INC 摘要:Provided herein are formulations, methods and substituted thieno[3,2-d]pyrimidine, furo[3,2-d]pyrimidine, and pyrrolo[3,2-d]pyrimidine compounds of Formula (I) for treating Pneumovirinae virus infections, including respiratory syncytial virus infections, as well as methods and intermediates for synthesis of substituted thieno[3,2-d]pyrimidine, furo[3,2-d]pyrimidine, and pyrrolo[3,2-d]pyrimidine compounds.
专利号:US-9701682-B2 优先权日:2013-11-11 标题:Pyrrolo[1,2-f][1,2,4]triazines useful for treating respiratory syncitial virus infections 发明人:CLARKE MICHAEL O'NEIL HANRAHAN; DOERFFLER EDWARD; MACKMAN RICHARD L; SIEGEL DUSTIN 权利人:GILEAD SCIENCES INC 摘要:Provided herein are formulations, methods and substituted tetrahydrofuranyl-pyrrolo[1,2-f][1,2,4]triazine-4-amine compounds of Formula (I) for treating Pneumovirinae virus infections, including respiratory syncytial virus infections, as well as methods and intermediates for synthesis of tetrahydrofuranyl-pyrrolo[1,2-f][1,2,4]triazine-4-amine compounds.