CAS: 89778-26-7; Toremifene

上下游产品

1,2-diphenyl-1-[4-[2-(N,N-dimethylamino)ethoxy]phenyl]butane-1,4-diol 4-hydroxy-1,2-diphenyl-1-[4-[2-N,N-dimethylamino]ethoxy]-phenyl-1-butene 4-Hydroxybenzophenone 3-hydroxy-1-phenylpropan-1-onetoremifene citrate

📜1,2-Diphenyl-1-[4-[2-(N,N-Dimethylamino)Ethoxy]Phenyl]Butane-1,4-Diol置于氯化亚砜,Sodium Hydroxide体系中,用 甲苯,水 作为反应溶剂,化学反应 14.0H,以40%的收率获得产物托瑞米芬
参考文献: Toremifene Crystallization Method[fr] Procede De Cristallisation De Toremifene
标题: Toremifene Crystallization Method[fr] Procede De Cristallisation De Toremifene
摘要:本发明涉及一种从托瑞米芬及其对应的e异构体混合物中分离托瑞米芬的方法.该方法包括将异构体混合物与第一溶剂(包括甲醇)接触,使托瑞米芬在该第一溶剂中结晶,然后将前一步骤中结晶的产物在第二溶剂(包括丙酮,甲乙酮或乙酸乙酯)中结晶,可选地将从前一步骤中结晶的托瑞米芬转化为其药学上可接受的盐.

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-7173021-B2
优先权日:2004-09-02
标题:Synthesis of temozolomide esters as potent anticancer pro-drugs for topical and transdermal applications in treatments of cancers
发明人：WANG YONGFENG; CONWAY BARBARA R; SUPPASANSATORN PANASSAYA
权利人:TIANJIN NORTH PHARM SCI TECH C
摘要:This invention relates to the use of temozolomide esters (4-dihydro-3-methyl-4-oxoimidazo[5,1-d]-1,2,3,5-tetrazine-8-carboxylate esters) Formula 1 as potent anticancer pro-drugs for treatment of cancers by topical and transdermal applications, and to a novel process for synthesis of temozolomide esters by a direct esterification of temozolomide acid (3,4-dihydro-3-methyl-4-oxoimidazo[5,1-d]-1,2,3,5-tetrazine-8-carboxylic acid) with a halogeno-aliphatic compound in presence of a base, or with an alcohol in presence of a dehydrate agent

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-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.

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

专利号:US-2025206736-A1
优先权日:2019-11-14
标题 :Synthesis of kras g12c inhibitor compound
发明人：CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN
权利人:AMGEN INC
摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.