CAS: 77992-44-0; (5-Bromopyridin-2-yl)Hydrazine

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5-溴-2-氯吡啶置于hydrazine Hydrate体系中,用 乙醇 作为反应溶剂,以97%的收率获得产物2-肼基-5-溴吡啶
参考文献:使用dmf及其衍生物作为单碳源的无金属[4 + 1]和[5 + 1]环化反应制备杂环
标题:使用dmf及其衍生物作为单碳源的无金属[4 + 1]和[5 + 1]环化反应制备杂环
摘要:1,2,4-三唑并[3,4-A]吡啶和相关的杂环以及取代的三嗪是在各种药物和农用化学试剂中普遍发现的支架.在这里,我们报告了一种高效且实用的方法,该方法使用dmf及其衍生物进行[4 + 1]和[5 + 1]环化反应,以制备这些杂环.这种无金属的反应利用了贮存稳定的dmf作作为反应溶剂和碳供体,使用咪唑氯化物作为催化剂的优势,温和的反应条件可耐受广泛的底物范围并替代.制备的3-未取代的1,2,4-三唑并[3,4-A]吡啶和衍生物允许在3-位进一步引入各种官能团.
DOI:10.1016/j.Tetlet.2020.151844

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-2006004188-A1
优先权日:2000-09-29
标 题:Intermediates and the synthesis of modified carbocyanine dyes and their conjugates

专利号:US-7566790-B2
优先权日:2000-09-29
标 题 :Intermediates and the synthesis of modified carbocyanine dyes and their conjugates

专利号:CN-113774411-A
优先权日:2021-09-22
标题 :A kind of method for electrochemical synthesis of aryl-substituted quinoxaline (ketone) derivatives

专利号:US-9938258-B2
优先权日:2012-11-29
标 题:Substituted 2,3-dihydrobenzofuranyl compounds and uses thereof
发明人：BALOGLU ERKAN; SHECHTER SHARON; SHACHAM SHARON; MCCAULEY DILARA; SENAPEDIS WILLIAM; GOLAN GALI; KALID ORI
权利人:KARYOPHARM THERAPEUTICS INC
摘要:The invention generally relates to substituted 2,3-dihydrobenzofuranyl compounds, and more particularly to a compound represented by Structural Formula I: n nor a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of Structural Formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment of cancer (e.g., mantle cell lymphoma), and other diseases and disorders.

专利号:CN-102002040-A
优先权日:2009-09-01
标 题:Synthesis method of triazol pyridine ring compound