CAS: 936250-20-3; 3-Methyl-4-(4,4,5,5-Tetramethyl-1,3,2-Dioxaborolan-2-yl)-1H-Pyrazole

相似化合物

1071455-14-5 1009071-34-4 857530-80-4

3-甲基吡唑,联硼酸频那醇酯置于(1,5-Cyclooctadiene)(Methoxy)Iridium(I) Dimer,3,4,7,8-四甲基-1,10-菲罗啉体系中,用 四氢呋喃 作为反应溶剂,化学反应 21.0H,以38%的收率获得产物3-甲基-1H-吡唑-4-硼酸频哪醇酯
参考文献:铱催化的杂芳烃的 C-H 硼化:范围,区域选择性,后期功能化的应用和机制
标题:铱催化的杂芳烃的 C-H 硼化:范围,区域选择性,后期功能化的应用和机制
摘要:报道了铱催化杂芳烃的 Ch 硼化的研究.发现几种含有多个杂原子的杂芳烃适合由铱 (I) 前体和四甲基菲咯啉的组合催化的 Ch 硼化.对反应范围的研究导致了预测硼化的区域选择性的强大规则的发展,其中最重要的是硼化发生在氮原子的远端.报告了原位形成的杂芳基硼酸酯的一锅官能化,证明了所报告的方法对合成复杂杂芳基结构的有用性.还展示了这种方法在生物活性化合物的合成和后期功能化中的应用.机理研究表明,碱性杂芳烃可以与催化剂结合,并将在芳烃硼化过程中观测到的烯烃结合复合物的静止状态改变为含有结合杂芳烃的物质,从而导致催化剂失活.对观测到的区域选择性起源的研究表明,由于快速的 Nh 硼酸化,硼酸化发生在 Nh 键的远端,为与这些键相邻的硼酸化创造了不利的空间环境.计算研究和机理研究表明,与碱性氮相邻的 Ch 键缺乏可观测到的硼化并不是在 Ch 活化之前与庞大的路易斯酸配位的结果,
DOI:10.1021/ja412563E

专利信息

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-8445510-B2
优先权日:2010-05-14
标题 :Fused bicyclic kinase inhibitors
发明人：MULVIHILL MARK J; STEINIG ARNO G; CREW ANDREW PHILIP; JIN MEIZHONG; KLEINBERG ANDREW; LI AN-HU; WANG JING
权利人:MULVIHILL MARK J; STEINIG ARNO G; CREW ANDREW PHILIP; JIN MEIZHONG; KLEINBERG ANDREW; LI AN-HU; WANG JING; OSI PHARMACEUTICALS LLC
摘要:Compounds of Formula I, as shown below and defined herein: n n n n n n n n n n pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven at least in part by at least one of RON, MET or ALK. This Abstract is not limiting of the invention.

专利号:US-9133224-B2
优先权日:2010-11-29
标 题:Macrocyclic kinase inhibitors
发明人：CREW ANDREW P; DONG HANQING; FERRARO CATERINA; SHERMAN DAN; SIU KAM W
权利人:CREW ANDREW P; DONG HANQING; FERRARO CATERINA; SHERMAN DAN; SIU KAM W; OSI PHARMACEUTICALS LLC
摘要:Compounds of Formula (I): wherein variables are defined herein, and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers for which FAK inhibition is beneficial.