1-乙酰基-5-硝基二氢吲哚置于sodium Hydroxide,Aluminium-Nickel Alloy体系中,用 水 作为反应溶剂,化学反应 1.5H,以56%的收率获得产物5-氨基吲哚 参考文献:Indole Derivatives. 131. The Basicity Of 5-And 6-Aminoindoles 标题:Indole Derivatives. 131. The Basicity Of 5-And 6-Aminoindoles 摘要: DOI:10.1007/bf00475595
专利信息
专利号:US-2022356182-A1 优先权日:2009-03-27 标题 :Inhibitors of hepatitis c virus replication 发明人:COBURN CRAIG A; LUDMERER STEVEN W; LIU KUN; WU HAO; SOLL RICHARD; ZHONG BIN; ZHU JIAN 权利人:MERCK SHARP & DOHME 摘要:The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
专利号:US-2024262834-A1 优先权日:2021-05-28 标 题:Synthesis of btk inhibitor and intermediates thereof 发明人:CHEN YONGGANG; CORRY JAMES; DESMOND RICHARD; DI MASO MICHAEL J; FORSTATER JACOB H; KUETHE JEFFREY T; KUHL NADINE; LARSON REED; LEVESQUE FRANCOIS; NARSIMHAN KARTHIK; OTTE DOUGLAS; PRIER CHRISTOPHER K; SHEVLIN MICHAEL; SIROTA ERIC; TAN LUSHI; THAISRIVONGS DAVID A; TURNBULL BEN W H; WANG ZHIXUN; XIAO KAIJIONG 权利人:MERCK SHARP & DOHME LLC 摘要:The present invention relates to efficient synthetic processes useful in the preparation of Compound A, a BTK inhibitor of Formula (I): or a pharmaceutically acceptable salt thereof, including the preparation of intermediates used to make Compound A or a pharmaceutically acceptable salt thereof.
专利号:US-12018251-B2 优先权日:2017-10-13 标 题:Method for synthesis of polynucleotides using a diverse library of oligonucleotides 发明人:VLADAR HAROLD PAUL; FERNANDES REDONDO RODRIGO APARECIDO 权利人:RIBBON BIOLABS GMBH 摘要:A method for synthesizing a target double stranded (ds) polynucleotide byproviding an oligonucleotide library within an array device that has a diversity of oligonucleotide library members, each of which has a different nucleotide sequence and is contained in a separate library containment in an aqueous solution. The library includes single stranded oligonucleotides and double stranded oligonucleotides with at least one overhang and covers at least 10,000 pairs of matching oligonucleotides. In a first step, at least a first pair of matching oligonucleotides are transferred transferred from the library into a first reaction containment using a liquid handler and the matching oligonucleotides are assembled, thereby obtaining a first reaction product comprising at least one overhang. Further reaction products are then likewise obtained and are assembled in a predetermined workflow using an algorithm, thereby producing said target ds polynucleotide with an overhang, optionally followed by a finalization step to prepare blunt ends.
专利号:US-9533959-B2 优先权日:2013-10-07 标 题:Methods of regioselective synthesis of 2,4-disubstituted pyrimidines 发明人:CHARRIER JEAN-DAMIEN; O'DONNELL MICHAEL EDWARD 权利人:VERTEX PHARMA 摘要:The present invention relates to the novel regioselective syntheses of 2,4-disubstituted pyrimidines through sequential nucleophilic aromatic substitutions.
专利号:US-11053243-B2 优先权日:2009-03-27 标 题:Inhibitors of hepatitis C virus replication 发明人:COBURN CRAIG A; LUDMERER STEVEN W; LIU KUN; WU HAO; SOIL RICHARD; ZHONG BIN; ZHU JIAN 权利人:MERCK SHARP & DOHME 摘要:The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
专利号:US-9090661-B2 优先权日:2009-03-27 标 题:Inhibitors of hepatitis C virus replication 发明人:COBURN CRAIG A; MCCAULEY JOHN A; LUDMERER STEVEN W; LIU KUN; VACCA JOSEPH P; WU HAO; HU BIN; SOLL RICHARD; SUN FEI; WANG XINGHAI; YAN MAN; ZHANG CHENGREN; ZHENG MINGWEI; ZHONG BIN; ZHU JIAN 权利人:MERCK SHARP & DOHME 摘要:The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
[参考文献]: Michael Jakun Koo, Et Al. Impaired Oxidative Phosphorylation Regulates Necroptosis In Human Lung Epithelial Cells. Biochem Biophys Res Commun. 2015 Aug 28;464(3):875-80.
合成参考文献
摘要:Harris, P. A., Science of Synthesis Knowledge Updates, (2021) 3, 41. 摘要:Ipaktschi, J.; Saidi, M. R., Science of Synthesis Knowledge Updates, (2012) 4, 417. 摘要:Hay, M. B.; Hicks, J. D., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 163. 摘要:Li, Y.; Fang, X.; Wang, Y., Science of Synthesis: DNA-Encoded Libraries, (2024) nan, 78. 参考文献:10.1021/jm030561b 摘要:Guengerich FP, Sorrells JL, Schmitt S, Krauser JA, Aryal P, Meijer L. Generation of new protein kinase inhibitors utilizing cytochrome p450 mutant enzymes for indigoid synthesis. J Med Chem. 2004 Jun 03;47(12):3236–41. doi: 10.1021/jm030561b.