CAS: 63612-50-0; 5,5-Dimethyl-3-(4-Nitro-3-(Trifluoromethyl)Phenyl)Imidazolidine-2,4-Dione

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CAS号400-74-8 2-氟-5-硝基三氟甲苯

在 1,8-二氮杂双环[5.4.0]十一碳-7-烯,1H-1,2,3-三氮唑体系中,用 乙酸乙酯 作为反应溶剂,化学反应 48.0H,以36.1%的收率获得产物尼鲁米特
参考文献:一种尼鲁米特及其中间体的制备方法
标题:一种尼鲁米特及其中间体的制备方法
摘要:本发明公开了一种尼鲁米特及其中间体的制备方法,该方法包括如下步骤:在温度为25oc至160°C,以式(ⅰ)4‑硝基‑3‑三氟甲基苯胺与带氨基保护基团pg的式(ⅱ)化合物为原料发生缩合和关环反应,分别反应生成式(ⅲ)化合物,式(Iii)不经纯化直接关环反应生成尼鲁米特(式ⅳ);或利用式(Iii)化合物关环制得尼鲁米特.本发明反应步骤短,操作简单,产率较高,反应条件温和,所用试剂廉价易得,既适合于实验室小规模制备,也适合于工业大规模生产.采用上述路线,为尼鲁米特的制备提供了一个新的构建乙内酰脲环的方法,对开发含此类结构的药物具有重要意义.

专利信息

专利号:US-11873305-B2
优先权日:2020-06-30
标题 :Processes for synthesis of substituted indole intermediates for the synthesis of serd compounds
发明人：ZHANG HAIMING; XU JIE; WUITSCHIK GEORG; ANGELAUD REMY; HEROLD SEBASTIAN; STUTZ ALFRED; BRUETSCH TOBIAS; BURKHARD JOHANNES
权利人:GENENTECH INC; HOFFMANN LA ROCHE
摘要:Provided herein are processes for the preparation of indolyl intermediates using Wenker Synthesis for the total synthesis of SERD compounds useful in the treatment of cancer.

专利号:US-12383499-B2
优先权日:2018-01-01
标题:Scale up synthesis of silicasome nanocarriers
发明人：NEL ANDRE E; MENG HUAN; LIU XIANGSHENG
权利人:UNIV CALIFORNIA
摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).

专利号:US-10925977-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
发明人：YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

专利号:US-2015239796-A1
优先权日:2014-02-19
标题:One pot synthesis of 18f labeledtrifluoromethylated compounds with difluoro(iodo)methane
发明人：RüHL THOMAS; RISS PATRICK; RAFIQUE WAQAS
权利人:UNIV OSLO
摘要:The present invention relates to compositions and methods for the synthesis of 18 F labeled compounds. In particular, the present invention relates to a copper (I) mediated one pot method for 18 F-trifluoromethylation of aromatic- or heteroaromatic halides with difluoro(iodo)methane (e.g., for use at PET imaging agents).

专利号:US-7700654-B2
优先权日:2005-02-05
标 题:Isolation of N-butylbenzenesulfonamide, synthesis of benzenesulfonamide derivatives, and use of N-butylbenzenesulfonamide and benzenesulfonamide derivatives for treating benign prostatic hyperplasia and/or prostate carcinoma
发明人：HOFFMANN HANS-RAINER; MATUSCH RUDOLF; BANIAHMAD ARIA
权利人:LOHMANN THERAPIE SYST LTS
摘要:A process for isolating N-butylbenzenesulfonamide (NBBS) from biological material, the chemical synthesis of benzenesulfonamide derivatives, the use of NBBS and benzenesulfonamide derivatives for treating benign prostatic hyperplasia and/or prostate carcinoma, the production of medicaments for the treatment thereof, and the use of NBBS and benzenesulfonamide derivatives as a lead substance in the development of active substances for treating benign prostatic hyperplasia and/or prostate carcinoma are provided.

专利号:US-12391691-B2
优先权日:2018-11-16
标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
发明人：PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
权利人:AMGEN INC
摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as