邻硝基苯硫酚置于盐酸,Sodium Hydroxide,双氧水,铁粉体系中,用 乙醇,水,溶剂黄146 作为反应溶剂,化学反应 20.25H,反应生成 2-(异丙基磺酰基)苯胺 参考文献:Notizen Zur Synthese Von 2-Aminophenylsulfonen 标题:Notizen Zur Synthese Von 2-Aminophenylsulfonen 摘要:某些烷基,环烷基和芳基2-氨基苯基砜的合成 DOI:10.1002/hlca.19800630610
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).
参考文献:10.1007/s11030-025-11259-7 摘要:Huo Y, Zhou Q, Zhang C, Lv Y, Liu R, Hou M, Duan X, Liu Y, Hu J. Design, synthesis and antitumor activity of thiadiazole derivatives as novel ALK kinase inhibitors. Mol Divers. 2026 Feb;30(1):1217–39. doi: 10.1007/s11030-025-11259-7.