CAS: 120511-73-1; Anastrozole

上下游产品

α,α,α',α'-tetramethyl-5-chloromethyl-1,3-benzene diacetonitrile anastrozole mesylate 2-[3-bromomethyl-5-(cyanodimethylmethyl)phenyl]-2-methylpropanenitrile sodium triazoleanastrozole mesylate 3,5-bis(2-cyanoprop-2-yl)toluene

2,2'-[5-(1H-1,2,4-Triazol-1-Ylmethyl)-1,3-Phenylene]-Di(2-Methylpropionitrile) Hydrobromide置于sodium Carbonate体系中,用 水 用作溶剂,以74.7%的收率获得阿那曲唑
参考文献:Novel Processes For Preparing Substantially Pure Anastrozole
标题:Novel Processes For Preparing Substantially Pure Anastrozole
摘要:本发明提供了一种新型的阿那曲唑纯化工艺,不需要使用液相色谱.纯化过程是通过分离的阿那曲唑盐形式实现的,可以通过结晶或选择性酸性萃取来实现,而且在这两种情况下都可以将纯化后的阿那曲唑盐转化为阿那曲唑碱.此外,本发明还提供了一种改进的合成阿那曲唑的工艺,该工艺通过烷基化分离和纯化起始材料3,5-双(2-氰基丙-2-基)苯基溴化物而获得,该过程不使用有毒,危险和环境不友好的溶剂和试剂.

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-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-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: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