CAS: 68047-06-3; (Z)-4-(1-(4-(2-(Dimethylamino)Ethoxy)Phenyl)-2-Phenylbut-1-En-1-yl)Phenol

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CAS号109517-76-2 (E)-1-[4-(benzy... | CAS号124-40-3 二甲胺 | CAS号611-99-4 4,4'-二羟基二苯甲酮 | CAS号68047-08-5 1-(4-(2-(dimeth... | CAS号93-55-0 苯丙酮 | CAS号185223-78-3 (E,Z)-1-[4-(ben... | CAS号440646-09-3 (E)-1-[4-(benzy... | CAS号1028310-31-7 4-benzyloxy-4'-... | CAS号76117-70-9 (E)-4-乙酰氧基他莫昔芬 | CAS号174592-47-3 (E)-4-羟基他莫昔芬

📜他莫昔芬置于n,N'-Dimethyl-N,N'-Bis(2-Pyridylmethyl)Ethane-1,2-Diamineiron(II) Bis(Triflate),双氧水,溶剂黄146体系中,用 乙酸乙酯,乙腈 作为反应溶剂,化学反应 24.0H,反应生成 4-羟基三苯氧胺
参考文献:Biomimetic Oxidation Of Aromatic Xenobiotics: Synthesis Of The Phenolic Metabolites From The Anti-Hiv Drug Efavirenz
标题:Biomimetic Oxidation Of Aromatic Xenobiotics: Synthesis Of The Phenolic Metabolites From The Anti-Hiv Drug Efavirenz
摘要:我们报道了一线抗 Hiv 药物依非韦伦 (Efv) 的氧化,该氧化是由仿生非血红素铁复合物介导的.根据实验条件,可以调整该系统以产生对映体纯形式的主要 Efv 代谢物 8-羟基-Efv,或模拟细胞色素 P450 (Cyp) 活性,产生 8-羟基-Efv 和 7-羟基-Efv,据报道在体内形成两种酚类 Efv 代谢物.抗雌激素他莫昔芬和马雌激素马烯雌酮成功氧化成其 Cyp 介导的代谢物,支持了仿生非血红素铁复合物在镜像 Cyp 活性中的普遍应用.
DOI:10.1039/c2Ob25212K

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-2015182634-A1
优先权日:2012-12-28
标 题:Molecular Design and Chemical Synthesis of Pharmaceutical-Ligands and Pharmaceutical-Pharmaceutical Analogs with Multiple Mechanisms of Action
发明人：COYNE CODY P; BEAR RYAN; JONES TONI
权利人:COYNE CODY P; BEAR RYAN; JONES TONI
摘要:Multi-phase and single-phase chemical reaction schemes have been developed for the synthesis of pharmaceutical-ligand analogs, pharmaceutical-pharmaceutical analogs, and similar molecular-molecular analogs that possess multiple mechanisms of action. The multi-phase organic chemical reaction schemes include relatively mild reaction conditions, high end product yields, and comparatively rapid completion of chemical reactions, which are all of particular utility for the synthesis of preparations including covalent pharmaceutical-receptor ligand or pharmaceutical-immunoglobulin analogs. Examples of pharmaceutical-ligand preparations that can be synthesized utilizing the multi-step chemical reaction schemes include covalent chemotherapeutic-ligand agents that possess selective targeted delivery properties and a capacity to exert additive and synergistic levels of cytotoxic anti-neoplastic potency. Pharmaceutical-pharmaceutical analogs, including chemotherapeutic-chemotherapeutic analogs that are capable of exerting multiple mechanisms of action, can be synthesized using either of the described multi-phase or single-phase organic chemistry reaction schemes. Each of these representative examples has utility against a spectrum of disease states including, for example, neoplastic conditions such as mammary adenocarcinoma/carcinoma, ovarian carcinoma, prostatic carcinoma, intestinal carcinoma, melanoma, leukemia, myeloma, and lymphoma.

专利号:WO-2017080770-A1
优先权日:2015-11-10
标题 :Synthesis of (z)-endoxifen hydrochloride
发明人：HEINKELE GEORG; MUERDTER THOMAS; SCHWAB MATTHIAS
权利人:ROBERT BOSCH GES FÃœR MEDIZINISCHE FORSCHUNG MBH
摘要:The invention relates to the synthesis of tamoxifen, endoxifen and derivatives thereof. Starting from a substituted benzoic acid derivative and 2-phenoxyethyl halide, the intermediate product of general formula (I) is obtained. The compound of general formula (VI) or a salt thereof is obtained from the compound of general formula (I), via isomer purification of the compound of general formula (I) by obtaining the (Z)-isomers and reacting the (Z)-isomers with an amine of formula HNR 6 R 7 . Alternatively, the compound of general formula (I) is reacted with a compound of formula HNR 6 R 7 , and the amine thus obtained is then subjected to isomer purification, wherein the compound of general formula (VI) or a salt thereof is obtained.

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-2008146656-A1
优先权日:2005-06-01
标题:Use of a steroid sulphatase inhibitor for inhibiting the synthesis of androstenedione and/or testosterone
发明人：REED MICHAEL JOHN; PUROHIT ATUL; WOO LOK WAI LAWRENCE; POTTER BARRY VICTOR LLOYD
权利人:REED MICHAEL JOHN; PUROHIT ATUL; WOO LOK WAI LAWRENCE; POTTER BARRY VICTOR LLOYD
摘要:There is provided use of a compound capable of inhibiting a steroid sulphatase enzyme (E.C.3.1.6.2) in the manufacture of a medicament for inhibiting in vivo synthesis of at least one of androstenedione and testosterone, which may be useful for the treatment of hirsutism, excess sebum production, benign breast disease, benign ovarian disease, polycystic ovarian disease and female infertility among others.