CAS: 107868-30-4; Exemestane

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CAS号19457-55-7 6-亚甲基雄-4-烯-3,17-二酮 | CAS号861395-77-9 ((8R,9S,10R,13S... | CAS号122370-91-6 亚甲基宝丹酮 | CAS号7440-44-0 活性炭 | CAS号75-65-0 叔丁醇 | CAS号846-48-0 宝丹酮 | CAS号897-06-3 1,4-雄烯二酮 | CAS号67737-88-6 1α,3-dipyrrolid... | CAS号53-43-0 去氢表雄酮 | CAS号184972-12-1 (8R,9S,10R,13S,...

6-Methyleneandrostenediol Ketal置于对甲苯磺酸体系中,用 四氢呋喃,水 用作溶剂,化学反应 10.0H,反应生成依西美坦
参考文献:依西美坦的制备方法
标题:依西美坦的制备方法
摘要:本发明依西美坦的制备方法涉及抗癌药物领域,具体涉及依西美坦的制备方法,包括以下步骤:6‑亚甲基雄二烯酮乙二醇缩酮的制备,在氮气保护下,依次将多聚甲醛,二甲胺盐酸盐和异戊醇加入到四口反应瓶中,加热回流带水2H,然后加入雄二烯酮乙二醇缩酮,于140度保温搅拌反应,高效液相色谱跟踪检测反应,15H反应结束,冷却至室温,加入蒸馏水水洗,分层后用无水硫酸镁干燥,减压回收溶剂,硅胶柱层析得白色固体;第二步,依西美坦的制备,在氮气保护下,依次将6‑亚甲基雄二烯酮乙二醇缩酮,对甲苯磺酸和四氢呋喃加入到四口瓶中;本发明工艺路线简捷,原料易得,成本低,收率高,且克服了现有技术存在的缺陷,适合工业化生产.

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-2005124592-A1
优先权日:2002-01-22
标 题:Tibolone in the treatment of complaints associated with the administration of drugs which prevent the synthesis of endogenous estrogen
发明人：KLOOSTERBOER HELENIUS J; BUNDRED NIGEL
摘要:Disclosed is a treatment of estrogen-deficiency related complaints in females that exhibit these complaints while they are on treatment with a drug which prevents the synthesis of endogenous estrogen. Such drugs are, e.g., anti-cancer drugs such as aromatase inhibitors. The invention resides in the use of tibolone, which has an unexpectedly beneficial working in this particular patient group in that it does not stimulate breast, while preventing bone loss and relieving climacteric complaints in a patient group in which this is more difficult than in any other group due to the nature of the concomitant cancer treatment (no circulating estrogen making for a higher severity of the complaints, the lack of effect on the estrogen receptor making for an increased risk associated with estrogenic breast stimulation once estrogen-like compounds are administered.

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:WO-2009034398-A1
优先权日:2007-09-11
标题:Process for the synthesis of 6-hydroxymethyl-l,4- androstadien-3.17-dione
发明人：HANTOS GABOR; HERINE BERTA MONIKA; TEGDES ANIKO; BARTHO ISTVAN; DEVENYI TAMAS; GALIK GYOERGY; PECSNE RAZSO AGNES; GANCSOS VALERIA; KOENCZOEL KALMAN; MAHO SANDOR
权利人:RICHTER GEDEON NYRT; HANTOS GABOR; HERINE BERTA MONIKA; TEGDES ANIKO; BARTHO ISTVAN; DEVENYI TAMAS; GALIK GYOERGY; PECSNE RAZSO AGNES; GANCSOS VALERIA; KOENCZOEL KALMAN; MAHO SANDOR
摘要:The invention relates to a novel process for the synthesis of 6-hydroxymethyl-l,4- androstadien-3,17-dione which means dehydrogenating 6-hydroxymethyl-4-androsten- 3,17-dione in the presence of a biocatalyst.

专利号:US-2021308144-A1
优先权日:2021-03-12
标 题:Synthesis of New Potent Aromatase Inhibitors Through Biocatalysis of Anti-Cancer Drugs, Atamestane, Drostanolone Enanthate, and Exemestane
发明人：WAHAB ATIA-TUL-; CHOUDHARY MUHAMMAD IQBAL; SIDDIQUI MAHWISH; SHAIKH NIMRA NAVEED; KHAN NISHA; RAHMAN ATTA-UR-
权利人:WAHAB ATIA TUL; CHOUDHARY MUHAMMAD IQBAL; SIDDIQUI MAHWISH; SHAIKH NIMRA NAVEED; KHAN NISHA; RAHMAN ATTA UR
摘要:New analogues of anti-cancer drugs atamestane (1), drostanolone enanthate ((3), and exemestane (6) were synthesized through biotransformation. New derivatives, 14α-hydroxy-1-methylandrosta-1,4-diene-3,17-dione ((2) (IC50, 9.7±0.72 nM) of 1 (IC50, 13.8±0.2 nM), and 2-methylandrosta-12β,17β-dihydroxy-1,4-diene-3-one (4) (IC50, 4.23±0.133 nM) of 3 (IC50, 6.4±0.06 nM) showed a potent inhibition against human aromatase enzyme and thus have the potential to treat ER+ breast-cancers and other related diseases. New metabolites, 2α-methyl-9α,17β-dihydroxy-5α-androstan-3-one ((5) (IC50=793.0±29.9 nM) of 3, 6-methylene-3α,7β,17β-trihydroxy-5β-androstane (7) (IC50, 46.1±0.81 nM), and 11α,17β-dihydroxy-6-methylene-androsta-1,4-diene-3-one (8) (IC5O=12797.0±844 nM) of exemestane (6) (IC50=232.0±31 nM) also showed a remarkable anti-aromatase activity. Aromatase is an enzyme, involves in the synthesis of estrogen (ER). Increased amount of ER due to overexpression of aromatase in the body, promotes cancerous cells growth in breast. Therefore, aromatase enzyme is a key target for the discovery of chemotherapeutic agents against ER+ breast-cancers.