CAS: 832114-00-8; 3,5-Dimethyl-4-(4,4,5,5-Tetramethyl-1,3,2-Dioxaborolan-2-yl)Isoxazole

上下游产品

3,5-二甲基异恶唑-4-硼酸 3,5-Dimethylisoxazole-4-Boronic Acid 16114-47-9

3,5-二甲基-4-碘基异恶唑,频那醇硼烷置于pdcl2(Pph3)2,Et3N体系中,用 1,4-二氧六环 作为反应溶剂,以67%的收率获得产物3,5-二甲基异恶唑-4-硼酸频哪醇酯
参考文献:Direct Conversion Of Pinacol Arylboronic Esters To Aryl Triolborates
标题:Direct Conversion Of Pinacol Arylboronic Esters To Aryl Triolborates
摘要:通过与1,1,1-三(羟甲基)乙烷(4)进行转酯化反应,将联苯酚芳基硼酸酯3转化为芳基三醇硼酸盐5的方法已被确立,其优点在于对各种官能团的耐受性.在二恶烷中,在moh(m = Na和k)和h2O的存在下,于30-60oc进行转酯化反应,获得了高产率的稳定芳基三醇硼酸盐5.
DOI:10.1246/cl.2011.702

专利信息

专利号:US-2018179191-A1
优先权日:2016-11-22
标题 :Synthesis of a compound that modulates the activity of bromodomain-containing proteins
发明人：SHEN JINYU; ST JULES MUSTAPHA; SPERANDIO DAVID; MOHAN SANKAR
权利人:GILEAD SCIENCES INC
摘要:The present disclosure provides processes for the preparation of a compound of formula I: n n n n n n n n n n or a salt or co-crystal thereof, that modulates the activity of bromodomain-containing proteins. The disclosure also provides compounds and processes for the preparation of the compounds that are synthetic intermediates to the compound of formula I.

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-2018097976-A1
优先权日:2016-11-22
标 题 :Synthesis of a compound that modulates the activity of bromodomain-containing proteins

专利号:US-12103929-B2
优先权日:2018-06-25
标题:Tricyclic compounds
发明人：FANG HAIQUAN; CHEN MINGMING; YANG GUIQUN; DU YUELEI; WANG YANPING; WU TONG; LI QINGLONG; ZHANG LEI; HU SHAOJING
权利人:JACOBIO PHARMACEUTICALS CO LTD
摘要:Disclosed are tricyclic compounds as bromodomain and extra-terminal (BET) inhibitors which are shown as formula I, their synthesis and their use for treating diseases. More particularly, disclosed are fused heterocyclic derivatives useful as inhibitors of BET, methods for producing such compounds and methods for treating diseases and conditions wherein inhibition of one or more BET bromodomains provides a benefit.

专利号:CN-117050075-A
优先权日:2022-05-05
标题:A class of biaromatic BET inhibitors and synthesis methods and uses