CAS: 108381-28-8; 4-(Benzyloxy)-2-Chloropyrimidine

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205672-19-1 81560-11-4 885952-28-3

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CAS号3934-20-1 2,4-二氯嘧啶 | CAS号100-51-6 苯甲醇

📜2,4-二氯嘧啶,苯甲醇置于potassium Tert-Butylate体系中,用 四氢呋喃,N,N-二甲基甲酰胺 用作溶剂,化学反应 13.5H,以76%的收率获得4-苄氧基-2-氯嘧啶
参考文献:Nhc配体周围的环缩合反应是合成高活性铃木-宫浦交叉偶联催化剂的关键步骤
标题:Nhc配体周围的环缩合反应是合成高活性铃木-宫浦交叉偶联催化剂的关键步骤
摘要:从2,4-二氯嘧啶开始,可通过五步反应序列获得4-(2-二烷基氨基)嘧啶基官能化的间苯二甲酰氯.已经找到了导致这些配体衍生的钯nhc配合物的两种途径:通过与相应的nhc-Agcl配合物进行重金属化,可以获得c,N配位的钯(II)配合物.在吡啶中和在k 2 Co 3存在下用咪唑鎓盐处理二氯化钯生成环金属化的化合物,从而得到c,C配位的化合物.详细研究了所有这些化合物的反应性及其在suzuki-Miyaura催化交叉偶联反应中的性能.结果表明,C,C配位的衍生物在芳基硼酸与芳基氯的偶联中表现出高催化活性,这与普遍接受的底物活化机理相一致.
Doi:10.1002/chem.201702877

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:WO-2025151642-A1
优先权日:2024-01-09
标题 :Modified elongation factor p and methods of use thereof
发明人：HECHT SIDNEY; DEDKOVA LARISA; POTUGANTI GAL REDDY; DASKALOVA SASHA
权利人:UNIV ARIZONA STATE
摘要:Provided herein are modified elongation factor P (EF-P) enzymes capable of incorporating noncanonical amino acids during protein synthesis at efficiencies that are different than those of native EF-P. Also provided are methods for preparing and using modified EF-P enzymes.