4-甲氧基吡啶-N-氧化物置于三氯氧磷体系中,化学反应 16.0H,反应生成2-氯-4-甲氧基吡啶 参考文献:Concise Total Syntheses Of Variolin B And Deoxyvariolin B 标题:Concise Total Syntheses Of Variolin B And Deoxyvariolin B 摘要:The Total Synthesis Of The Marine Alkaloid Variolin B Has Been Achieved In 8 Steps And 17% Overall Yield,Starting From Commercially Available 4-Chloro-2-Methylthiopyrimidine. The Key Reaction Involves The Tandem Deoxygenation And Cyclization Of A Triarylmethanol Using A Combination Of Triethylsilane And Trifluoroacetic Acid. In Addition,The Deoxygenated Analogue Was Prepared In 6 Steps And 23% Overall Yield,Starting From The Same Starting Material. Doi:10.1021/jo050523V
专利号:WO-2023091726-A1 优先权日:2021-11-18 标题:Inhibitors of cyclin‑dependent kinase 12 (cdk12) 发明人:BENOIT GUILLAUME; CARULLI JOHN; CHEN FEI; CHUAQUI CLAUDIO; CIBLAT STEPHANE; COOPER ELLIOT; DAGENAIS ROBIN; HU SHANHU; KABRO ANZHELIKA; LAPLACA DEREK; MARINEAU JASON; MOEBIUS DAVID; MOON DIANE; SOLODININ ANDREI; WHITMORE KENNETH 权利人:SYROS PHARMACEUTICALS INC 摘要:The present invention provides chemical compounds that inhibit one or more families of kinases (e.g., serine/threonine kinases, including one or more of the families of CDK proteins, and in particular, CDK12). More specifically, the present invention provides CDK12 inhibitors, of formula (I), pharmaceutically acceptable salts and isotopically labeled derivatives thereof, pharmaceutical compositions containing the compounds/inhibitors, and methods of their synthesis and use in treating proliferative diseases (e.g., a bladder cancer, a breast cancer, Ewing's sarcoma, a gastric cancer, a gastrointestinal cancer, a hematologic cancer, a lung cancer (e.g., small cell lung cancer (SCLC)), an ovarian cancer (e.g., a high grade serous ovarian cancer), a pancreatic cancer (e.g., pancreatic ductal adenocarcinoma (PDAC)), a brain cancer (e.g., glioblastoma), or a prostate cancer), alone or in combination with a second therapeutic agent. The proliferative disease can be a cancer, benign neoplasm, or pathologic angiogenesis, and any of the therapeutic methods or uses described herein can include a step of diagnosing the patient's disease. In other embodiments of the invention, the compositions described herein (e.g., the compounds, pharmaceutical compositions, and kits containing them) are used for the treatment of myotonic dystrophy (type 1 or type 2).
专利号:US-7999090-B2 优先权日:2000-07-07 标 题:Fungal cell wall synthesis gene 发明人:TSUKAHARA KAPPEI; HATA KATSURA; SAGANE KOJI; NAKAMOTO KAZUTAKA; TSUCHIYA MAMIKO; WATANABE NAOAKI; OHBA FUMINORI; TSUKADA ITARU; UEDA NORIHIRO; TANAKA KEIGO; KAI JUNKO 权利人:EISAI R&D MAN CO LTD 摘要:The present invention provides isolated DNA encoding a GWT1 protein having activity to confer resistance of a fungus against a compound of formula Ia, and wherein a defect of a function of the GWT1 protein leads to a decrease in the amount of a glycosylphosphatidylinositol (GPI)-anchored protein in the cell wall of a fungus.
专利号:MX-2008013487-A 优先权日:2000-07-07 标 题 :SYNTHESIS GEN OF THE FUNGAL CELL WALL.
参考标题:A Four-Coordinate Cu(I)-N-Heterocyclic Carbene Complex: Synthesis, Structure, Properties, And Application In Amination For The Synthesis Of 1-(2-N-Heteroaryl)-1H-Pyrazoles 作者:Chen Xu,Hong-Mei Li,Zhi-Qiang Wang,Wei-Jun Fu |发布日期:2020.11 摘要:A New Luminescent, Cationic, Heteroleptic, Four-Coordinate Cu(I)-N-Heterocyclic Carbene Complex [cu(Br-Pyim)(Pop)](Pf6) Is Successfully Prepared And Characterized, Where Br-Pyim And Pop Are 1-(6-Bromopyridin-2-Yl)Imidazole-3-Benzyl-2-Ylidene And Bis[2-(Diphenylphosphino)Phenyl]Ether, Respectively. Its Detailed Structure Is Determined By Single-Crystal X-Ray Analysis. It Exists As A Crystalline Powder
合成参考文献
摘要:Spitzner, D., Science of Synthesis Knowledge Updates, (2016) 1, 235. 摘要:Harsanyi, A.; Sandford, G., Science of Synthesis Knowledge Updates, (2015) 1, 161. 摘要:A.R. Katritzky, J.D. Rowe and S.K. Roy. J. Chem. Soc., B 1967, 758.