CAS: 2998-57-4; Estramustine

该化合物是一种合成化合物,主要用于治疗前列腺癌,主要用于治疗雌激素和氮芥子的特性;被归类为抗乳胶剂,通过干扰癌症细胞的生长和扩散发挥作用; 雌激素的化学结构具有类固醇核,经过修改以增强其治疗效果; 通常通过口服施用,并因其与雌激素受体结合的能力而为人所知,这可能有助于其抗癌活动; 雌激素还具有水溶性相对较低的特点,可影响其生物利用率; 与使用该物质相关的共同副作用包括胃肠紊乱,疲劳和因其食性活动而可能造成的荷尔蒙变化; 与许多止血药剂一样,仔细监测对于管理不利影响和评估治疗效果至关重要;

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CAS号2998-56-3 N,N-双(2-氯乙基)氨基甲酰氯 | CAS号50-28-2 雌二醇 | CAS号62899-40-5 Leo 271 f | CAS号50-28-2 雌二醇 | CAS号53-16-7 雌酚酮

合成工艺路线路线简述

  • 合成目标产物 Estramustine 主要起始原料 N,N-Bis(2-Chloroethyl)Carbamoyl Chloride And β-Estradiol
  • (文献来源)合成步骤主要原料 N,N-Bis(2-Chloroethyl)Carbamoyl Chloride 和 β-Estradiol
雌二醇氮芥置于镍 氢气体系中,化学反应生成雌莫司汀
参考文献:潜在的抗癌药.二.某些自然性激素的尿烷型氮芥.
标题:潜在的抗癌药.二.某些自然性激素的尿烷型氮芥.
摘要:
Doi:10.1021/jm00314A009

海关参考信息

专利信息


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-2012177593-A1
优先权日:2009-07-20
标 题 :Synthesis of dendrimer conjugates
发明人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH
权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN
摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.

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-10973847-B2
优先权日:2017-06-30
标题 :Core-to-surface polymerization for the synthesis of star polymers and uses thereof
发明人:JOHNSON JEREMIAH A; GOLDER MATTHEW R
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:Disclosed are methods, compositions, reagents, systems, and kits to prepare star polymers, as well as compositions and uses thereof. Various embodiments show that synthesis of these polymers contain low metal concentration to provide polymers for diverse biomedical applications including in vivo applications.

专利号:US-2025090698-A1
优先权日:2018-11-27
标题 :Small molecule inhibitors for early diagnosis of prostate specific membrane antigen cancers and neurodegenerative diseases
发明人:CHELVAM VENKATESH; SENGUPTA SAGNIK; KRISHNAN MENA ASHA; PANDIT AMIT
权利人:INDIAN INSTITUTE OF TECH INDORE
摘要:Accordingly, embodiments herein disclose a conjugate D-E-F having binding affinity≤60 nM; wherein D comprises AAPT ligand or derivative thereof, E comprises a spacer comprising AA1, AA2, AA3 and/or AA4 and F is a chelating group. The conjugate also comprising AAPT ligand conjugated arene chelating linker for delivery of 99mTc radioisotope. Another embodiment also discloses a AAPT-PCa DOTA bioconjugate. An embodiment also discloses method of solid phase synthesis of AAPT-ligand. It also discloses a method of solid phase synthesis of AAPT-PCa DOTA bioconjugate for delivering of radioisotopes.

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
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主要参考文献


1: Bissinger R, Modicano P, Frauenfeld L, Lang E, Jacobi J, Faggio C, Lang F. Estramustine-induced suicidal erythrocyte death. Cell Physiol Biochem. 2013;32(5):1426-36. doi: 10.1016/j.acuro.2013.07.010. Epub 2014 Feb 5. English, Spanish. Weekly, low-dose docetaxel combined with estramustine for Japanese castration-resistant prostate cancer: its efficacy and safety profile compared with tri-weekly standard-dose treatment. Int J Clin Oncol. 2014 Feb;19(1):165-72. doi: 10.1007/s10147-013-0536-7. Epub 2013 Mar 1. doi: 10.1097/MD.0000000000004801. Review.
5: Petrioli R, Roviello G, Fiaschi AI, Laera L, Bianco V, Ponchietti R, Barbanti G, Francini E. Low-Dose Estramustine Phosphate and Concomitant Low-Dose Acetylsalicylic Acid in Heavily Pretreated Patients With Advanced Castration-Resistant Prostate Cancer. Clin Genitourin Cancer. 2015 Oct;13(5):441-6. doi: 10.1016/j.clgc.2015.03.004. Epub 2015 Mar 26. doi: 10.1007/s10147-012-0463-z. Epub 2012 Aug 31. doi: 10.1007/s10147-012-0429-1. Epub 2012 Jun 12. doi: 10.1007/s12032-013-0717-2. Epub 2013 Sep 5. doi: 10.1111/j.1464-410X.2011.10201.x. Epub 2011 Jul 14. Review. doi: 10.1016/j.ejmech.2013.07.007. Epub 2013 Jul 27. doi: 10.1016/j.ejca.2011.10.015. Epub 2011 Nov 24. doi: 10.1007/s12032-012-0178-z. Epub 2012 Feb 10. doi: 10.1007/s00432-011-1052-7. Epub 2011 Sep 14. doi: 10.1016/j.bmcl.2010.11.117. Epub 2010 Dec 4.
16: Edgren M, Westlin JE, Letocha H, Nordgren H, Kälkner KM, Nilsson S. Estramustine-binding protein (EMBP) in renal cell carcinoma immunohistochemistry, immunoscintigraphy and in vitro estramustine effects. Acta Oncol. 1996;35(4):483-8. doi: 10.1016/j.urolonc.2009.09.012. Epub 2009 Dec 21. Review. Review.

合成参考文献


摘要:S10 | SWISSPHARMA | Pharmaceutical List with Consumption Data | DOI:10.5281/zenodo.2623484
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