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CAS号52334-81-3 2-氯-5-三氟甲基吡啶 | CAS号505084-59-3 2-氯-5-三氟甲基烟酸 | CAS号505084-56-0 2-氯-3-碘-5-(三氟甲基)吡啶 | CAS号505084-58-2 2-氯-5-三氟甲基吡啶-4-甲酸 | CAS号131747-40-5 5-三氟甲基烟酸2-氯-5-三氟甲基吡啶置于二异丙胺,Lithium Bromide,Lithium N,N-Diisopropylcarbamate,碘体系中,用 四氢呋喃,正己烷 作为反应溶剂,化学反应 2.75H,以67%的收率获得产物2-氯-5-三氟甲基-4-碘吡啶
参考文献:三氟甲基取代的吡啶羧酸和喹啉羧酸的推荐路线
标题:三氟甲基取代的吡啶羧酸和喹啉羧酸的推荐路线
摘要:作为案例研究的一部分,准备的合理策略.所有 10 种 2-,3-或 4-吡啶羧酸和所有 9 种在 2-,3-或 4-位带有三氟甲基取代基的 2-,3-,4-或 8-喹啉羧酸中的 如果前体中尚未存在三氟甲基,则通过用四氟化硫对合适的羧酸进行脱氧氟化或通过原位反应生成的三氟甲基铜置换环结合的溴或碘来引入三氟甲基.羧基功能是通过用二氧化碳处理有机锂或有机镁中间体,卤素/金属或氢/金属置换的产物而产生的.[在 Scifinder (R) 上]
DOI:10.1002/ejoc.200390215
海关参考信息
- 2933310010-吡啶
2903399090-其他无环烃卤化衍生物
2939800000-其他生物碱 - 💡 提示:海关信息按照顺序优先匹配,如需确认的海关信息,请参考相关资料。
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专利信息
专利号:US-9505719-B2
优先权日:2010-06-30
标 题 :Synthesis and use of kinase inhibitors
发明人:LEI YIXIONG; BEHRENS CARL HENRY; LI HUI-YIN; SUN CONNIE L
权利人:VERASTEM INC
摘要:An improved synthesis of a class of inhibitor of Focal Adhesion Kinase (FAK) is provided, wherein use of an expensive palladium-based catalyst is reduced and reaction yields and product purities are improved. Two key reactions of coupling of aryl halides with anilines are optimized with the surprising discovery that the palladium-based catalyst can be dispensed with entirely in one of the reactions. The invention also provides the use of the FAK-inhibitory compounds in the treatment of inflammatory and immune disorders and of arthritis.
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:CA-2803005-A1
优先权日:2010-06-30
标 题 :Synthesis and use of kinase inhibitors
专利号:WO-2012012139-A1
优先权日:2010-06-30
标题:Synthesis and use of kinase inhibitors
专利号:EP-2588476-A1
优先权日:2010-06-30
标题 :Synthesis and use of kinase inhibitors
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.