N,N-二甲基甲酰胺置于正丁基锂体系中,用 四氢呋喃,正己烷 用作溶剂,化学反应 1.5H,反应生成2-氟-4-甲氧基苯甲醛 参考文献:1-Substituted-3-Beta-D-Glycopyranosylated Nitrogenous Hetero-Cyclic Compounds And Medicines Containing The Same 标题:1-Substituted-3-Beta-D-Glycopyranosylated Nitrogenous Hetero-Cyclic Compounds And Medicines Containing The Same
专利号:US-9796641-B2 优先权日:2013-03-22 标 题:Stabilization of radiosynthetic intermediates 发明人:OTABASHI MUHAMMAD; PHILIPPART GAUTHIER; VOCCIA SAMUEL; WOUTERS LUDOVIC; MORELLE JEAN-LUC 权利人:TRASIS S A 摘要:The present invention relates to a method for stabilizing radiosynthetic intermediates used in synthesis of 18 F radiolabeled aromatic amino acid derivatives toward decomposition caused by beta and gamma radiations by the use of radical scavengers and/or reductants and/or antioxidants.
专利号:US-10793557-B2 优先权日:2018-04-03 标题 :Sting agonist compounds 发明人:ALTMAN MICHAEL D; CASH BRANDON D; CHILDERS MATTHEW LLOYD; CUMMING JARED N; DEMONG DUANE E; HAIDLE ANDREW MARC; HENDERSON TIMOTHY J; JEWELL JAMES P; LARSEN MATTHEW A; LIM JONGWON; LU MIN; OTTE RYAN D; TROTTER BENJAMIN WESLEY 权利人:MERCK SHARP & DOHME 摘要:Compounds of general formula (I), of general formula (II), of general formula (III), of general formula (IV), of general formula (V), of general formula (VI), and their pharmaceutically acceptable salts, wherein all variables are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are compositions comprising such compounds, processes for the synthesis of such compounds, and to uses of such compounds, including administration of such compounds to induce immune response, to induce STING-dependent type I interferon production, and/or to treat a cell proliferation disorder, such as cancer.
专利号:US-8633182-B2 优先权日:2012-05-30 标题:Indanyloxyphenylcyclopropanecarboxylic acids 发明人:HAMPRECHT DIETER; FRATTINI SARA; LINGARD IAIN; PETERS STEFAN 权利人:HAMPRECHT DIETER; FRATTINI SARA; LINGARD IAIN; PETERS STEFAN; BOEHRINGER INGELHEIM INT 摘要:The present invention relates to compounds of general formula I, n nwherein the groups R 1 , R 2 , R 3 , m and n are defined as in claim 1 , which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.
专利号:US-8927560-B2 优先权日:2010-12-06 标 题 :4-Aza-2, 3-didehydropodophyllotoxin compounds and process for the preparation thereof 发明人:AHMED KAMAL; PAIDAKULA SURESH; BANALA ASHWINI KUMAR; ADLA MALLAREDDY; PAPAGARI VENKAT REDDY; JAKI RASHEED TAMBOLI 权利人:AHMED KAMAL; PAIDAKULA SURESH; BANALA ASHWINI KUMAR; ADLA MALLAREDDY; PAPAGARI VENKAT REDDY; JAKI RASHEED TAMBOLI; COUNCIL SCIENT IND RES 摘要:The present invention provides 4-Aza-2,3-didehydropodophyllotoxin compound of general formula A (4a-4z and 4aa-4ae) as useful potential antitumour agents against human cancer cell lines. The present invention further provides a process for the synthesis of 4-Aza-2,3-didehydropodophyllotoxin compounds (4a-4z and 4aa-4ae).
专利号:WO-0050406-A1 优先权日:1999-02-22 标 题 :Isoquinoline derivatives and isoquinoline combinatorial libraries 发明人:LEBL MICHAEL 权利人:TREGA BIOSCIENCES INC 摘要:The present invention provides the synthesis of heterocyclic compounds based on the isoquinoline ring. More specifically, the invention provides novel isoquinoline derivatives as well as novel libraries comprised of such compouds.
专利号:US-9423395-B2 优先权日:2013-01-14 标 题:Fluorescent cell cycle probe having M-phase specificity 发明人:CHANG YOUNG-TAE; ZHAI DUANTING; LEE SUNG-CHAN; YUN SEONG-WOOK; JEONG YUN-MI; KANG NAM-YOUNG; PARK SUNG-JIN 权利人:NAT UNIV SINGAPORE; AGENCY SCIENCE TECH & RES 摘要:The present invention is directed to a novel family of fluorophores based on the BODIPY scaffold, and methods for their synthesis. The BODIPY-based fluorophores disclosed herein are used for the selective visualization of cells that exist in the M-phase of the cell cycle. The present invention further relates to methods for the image-based monitoring of mitotic progression in live cells.
[参考文献]: Jack G Parsons, Et Al. Chiral Building Blocks: Enantioselective Syntheses Of Benzyloxymethyl Phenyl Propionic Acids. Molecules. 2004 May 31;9(6):449-58.
合成参考文献
摘要:Sapeta, K.; Kerr, M. A., Science of Synthesis Knowledge Updates, (2011) 1, 18. 摘要:Chan, W.-W.; Yu, W.-Y., Science of Synthesis: Catalytic Transformations via CH Activation, (2015) 2, 101.