三氟(4-(甲基磺酰基)苯基)硼酸盐 以 Phosphate Buffer 用作溶剂,化学反应生成4-(甲磺酰基)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-11767302-B2 优先权日:2020-10-01 标题 :Reagents and methods for tetrazine synthesis 发明人:FOX JOSEPH M; LAMBERT WILLIAM; FANG YINZHI; AM ENDE CHRISTOPHER WILLIAM; MAHAPATRA SUBHAM; XIE YIXIN; WANG CHUANQI 权利人:UNIV DELAWARE 摘要:Disclosed herein are mono- and di-substituted tetrazines and methods of their preparation and converting an oxetanyl ester to a thio-substituted tetrazine, which is then converted to a mono-substituted tetrazine, a di-substituted tetrazine, or a vinylether disubstituted tetrazine.
专利号:US-9308194-B2 优先权日:2013-11-28 标 题:Indanyloxyphenylcyclopropanecarboxylic acids 发明人:LINGARD IAIN; HAMPRECHT DIETER 权利人:BOEHRINGER INGELHEIM INT 摘要:A compound of formula I, n nwherein the groups R 1 , R 2 , R 3 , X, 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-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:US-2007275968-A1 优先权日:2004-09-07 标 题 :Substituted Biphenyl Derivative 发明人:KURATA HITOSHI; NISHIMATA TOYOKI; WATANABE YUKIKO; EBISAWA MASAYUKI; FUJIMOTO TEPPEI; KOBAYASHI HIDEKI 权利人:KURATA HITOSHI; NISHIMATA TOYOKI; WATANABE YUKIKO; EBISAWA MASAYUKI; FUJIMOTO TEPPEI; KOBAYASHI HIDEKI 摘要:The present invention relates to a biaryl derivative or a pharmacologically acceptable salt thereof having an excellent collagen-synthesis inhibition activity. A biaryl derivative having a structure represented by the following General Formula (I) or a pharmacologically acceptable salt thereof: n nwherein n R 1 represents a C 6 -C 10 aryl group which is substituted with one to three group(s) each independently selected from the group consisting of a group defined by formula R-L-, a di-(C 1 -C 6 alkyl)amino group, a di-(C 1 -C 6 alkyl)aminosulfonyl group, a hydroxyaminocarbonyl group, and a halogen atom, and so on; R represents a C 1 -C 6 alkyl group, and so on; L represents a sulfonyl group, an aminosulfonyl group, or a sulfonylamino group, and so on; R 2 represents a hydrogen atom, and so on; A represents a group defined by formula (II), (III), or (IV); R 3 represents a C 1 -C 6 alkyl group, and so on; and R 4 represents a C 1 -C 6 alkyl group, and so on.
摘要:Giel, M.-C.; Smedley, C. J.; Moses, J. E., Science of Synthesis, (2021) , 451. 摘要:Li, J. J., Science of Synthesis: Knowledge Updates, (2025) 2. 摘要:Xu, C.; Shao, X.; Shen, Q., Science of Synthesis: Modern Strategies in Organofluorine Chemistry , (2024) 1, 32.