(2,4-Dichlorophenyl)-Trifluoroboranuide 以 Phosphate Buffer 作为反应溶剂,化学反应生成 2,4-二氯苯硼酸 参考文献:Substituent Effects On Aryltrifluoroborate Solvolysis In Water: Implications For Suzuki−miyaura Coupling And The Design Of Stable 18F-Labeled Aryltrifluoroborates For Use In Pet Imaging 标题:Substituent Effects On Aryltrifluoroborate Solvolysis In Water: Implications For Suzuki−miyaura Coupling And The Design Of Stable 18F-Labeled Aryltrifluoroborates For Use In Pet Imaging 摘要:Whereas Electron Withdrawing Substituents Retard The Rate Of Aryltrifluoroborate Solvolysis,Electron-Donating Groups Enhance It. Herein Is Presented A Hammett Analysis Of The Solvolytic Lability Of Aryltrifluoroborates Where Log(K(Solv)) Values Correlate To Sigma Values With A Rho Value Of Approximately-1. This Work Provides A Predictable Rubric For Tuning The Reactivity Of Boron For Several Uses Including F-18-Labeled Pet Reagents And Has Mechanistic Implications For Arbf3-Enhanced Ligandless Metal-Mediated Cross Coupling Reactions With Aryltrifluoroborates. DOI:10.1021/jo800681D
专利号:US-12150934-B2 优先权日:2016-11-30 标 题 :Methods of using substituted pyrazole and pyrazole compounds and for treatment of hyperproliferative diseases 发明人:SIDDIQUI ARSHAD M; CIBLAT STEPHANE; CONSTANTINEAU-FORGET LEA; GRAND-MAITRE CHANTAL; GUO XIANGYU; SRIVASTAVA SANJAY; SHIPPS GERALD W; COOPER ALAN B; OZA VIBHA; KOSTURA MATTHEW W; LUTHER MICHAEL; LEVINE JEDD 权利人:BANTAM PHARMACEUTICAL LLC 摘要:Disclosed are methods of treating hyperproliferative disorders such as cancer, methods of arresting the cell cycle in cancer cells, methods of inhibiting glutathione synthesis in cancer cells, and associated compounds for use and uses in medicaments. In certain embodiments, the methods, uses and compounds are provided with reference to compounds of the structural formula (I), in which X1, X2, Z1, Z2, the ring system denoted by “aâ€?, R1, L1, L2, Q, L3, R3, L4, R4, L5, and R5 are as described herein. In certain embodiments, compounds disclosed herein are especially active against cancers having a mutant KRAS gene.
专利号:US-7781470-B2 优先权日:1999-09-13 标题:Aminodicarboxylic acid derivatives having pharmaceutical properties 发明人:ALONSO-ALIJA CRISTINA; HEIL MARKUS; FLUBACHER DIETMAR; NAAB PAUL; PERNERSTORFER JOSEF; STASCH JOHANNES-PETER; WUNDER FRANK; DEMBOWSKY KLAUS; PERZBORN ELIZABETH; STAHL ELKE 权利人:BAYER SCHERING PHARMA AG 摘要:The invention relates to compounds of formulae (II), (IV), and (VI) as shown below, n nwherein the several variable groups are as defined in the specification and claims. Processes for making these materials, and methods for using them in the synthesis of compounds for treatment of cardiovascular disorders and fibrotic disorders are also disclosed.
专利号:US-8383643-B2 优先权日:2009-07-28 标题 :Spiro compounds useful as inhibitors of stearoyl-coenzyme A delta-9 desaturase 发明人:LECLERC JEAN-PHILIPPE; LI CHUN-SING; MORADEI OSCAR MIGUEL 权利人:MERCK CANADA INC; LECLERC JEAN-PHILIPPE; LI CHUN-SING; MORADEI OSCAR MIGUEL 摘要:Heteroaromatic compounds of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.
专利号:US-9988371-B2 优先权日:2014-06-03 标 题:Benzimidazole analogues and related methods 发明人:LI HONG-YU; FRETT BRENDAN; SANTORO MASSIMO; CARLOMAGNO FRANCESCA 权利人:UNIV ARIZONA; UNIV FEDERICO II; UNIV ARIZONA 摘要:The invention relates to compounds of the formula (VIII) wherein the moieties R 1 , R 2 , R 3 , R 4 , and R 5 are as defined in the specification, and salts thereof, as well as their use, methods of use for them, methods of their synthesis, and the like. The compounds are protein tyrosine kinase inhibitors and can be used in the treatment of various cancer diseases and cancer-associated pain.
专利号:US-2025026766-A1 优先权日:2022-01-12 标题 :Thiazolopyridyl Amide Derivatives as DNA Polymerase Theta Inhibitors 发明人:LI JING; XU WENQING; WANG ZHIWEI 权利人:BEIGENE LTD 摘要:The present invention relates to compounds containing thiazolopyridyl amide structure, the process for their synthesis, as well as the use of such compounds for inhibiting DNA Polymerase Theta (Pol Theta), and in the treatment of various diseases including cancers.
专利号:CN-114805015-A 优先权日:2022-06-07 标题 :Synthesis process of 2,4-dichloro-9,9-dimethyl-9H-fluorene