CAS: 722533-56-4; Elacestrant

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参考文献:Selective Estrogen Receptor Modulator
标题:Selective Estrogen Receptor Modulator
摘要:本发明提供一种由以下式(i)表示的化合物; [其中t表示单键,可能具有取代基的c1-C4烷基和类似物;式(i-1)表示单键或双键;a表示单键,可能具有取代基的双价5-至14-成员杂环基和类似物;y表示单键和类似物;z表示亚甲基基团和类似物;环g表示苯基团和类似物,可能与5-至6-成员环缩合并可能具有杂原子;ra和rb相同或不同,表示氢原子和类似物;w表示单键和类似物;r'表示1到4个独立的氢原子和类似物;r''表示1到4个独立的氢原子和类似物]或其盐或水合物.

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:WO-2025132864-A1
优先权日:2023-12-21
标 题:Enantioselective synthesis of elacestrant intermediates
发明人：CALVANI FEDERICO; MORINI FRANCESCA; D'ARATA FABIO; MASI MATTEO; RAMACCIOTTI ALESSIO; SCHMITZ REINHARD; BONACCORSI FABRIZIO
权利人:BERLIN CHEMIE AG
摘要:An improved synthesis of (R)-6-(2-amino-4-methoxyphenyl)-5,6,7,8-tetrahydronaphtalen-2-ol proceeds by three steps: (1) enantioselective catalytic hydrogenation to form a compound of Formula (IV'); (2) catalytic hydrogenation to form a compound of Formula (IX); and (3) acid hydrolysis to obtain (R)-6-(2-amino-4-methoxyphenyl)-5,6,7,8-tetrahydronaphtalen-2-ol in high 5 yield (greater than 70%) and high optical purity of the (R) enantiomer (90% or greater).

专利号:US-2024174678-A1
优先权日:2020-06-30
标 题 :Processes for synthesis of substituted indole intermediates for the synthesis of serd compounds

专利号:WO-2024165901-A1
优先权日:2023-02-06
标题 :BENZO[b]SELENOPHENES AS NOVEL SELECTIVE ESTROGEN RECEPTOR MODULATORS
发明人：ARSENJANS PAVELS; PAEGLE EDGARS
权利人:LATVIAN INST ORGANIC SYNTHESIS
摘要:The present invention relates to a novel benzoselenophenes as anticancer agents by modulating estrogen receptor alpha (ERα) activity, as well as methods of their manufacturing and use in different pharmaceutical compositions for the treatment of various diseases and disorders by administration of such substances.

专利号:US-11780834-B2
优先权日:2018-06-21
标题:Solid forms of 3-((1R,3R)-1-(2,6-difluoro-4-((1-(3-fluoropropyl)azetidin-3- yl)amino)phenyl)-3-methyl-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indol-2-yl)-2,2-difluoropropan-1-ol and processes for preparing fused tricyclic compounds comprising a substituted phenyl or pyridinyl moiety, including methods of their use
发明人：CHUNG CHEOL KEUN; XU JIE; IDING HANS; CLAGG KYLE; DALZIEL MICHAEL; FETTES ALEC; GOSSELIN FRANCIS; LIM NGIAP-KIE; MCCLORY ANDREW; ZHANG HAIMING; CHAKRAVARTY PAROMA; NAGAPUDI KARTHIK; ROBINSON SARAH
权利人:HOFFMANN LA ROCHE; GENENTECH INC
摘要:Provided herein are solid forms, salts, and formulations of 3-((1R,3R)-1-(2,6-difluoro-4-((1-(3-fluoropropyl)azetidin-3-yl)amino)phenyl)-3-methyl-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indol-2-yl)-2,2-difluoropropan-1-ol, processes and synthesis thereof, and methods of their use in the treatment of cancer.

专利号:WO-2025077502-A1
优先权日:2023-10-09
标题:Asymmetric catalytic hydrogenation method for cyclohexene derivatives
发明人：ZHANG WANBIN; CHU DINGJUN; YUAN QIANJIA; XIE XIAOQIANG
权利人:AURISCO PHARMACEUTICAL CO LTD; UNIV SHANGHAI JIAOTONG
摘要:The present invention provides an asymmetric catalytic hydrogenation method for a compound as shown in formula (I), comprising the following steps: in a hydrogen atmosphere, performing asymmetric hydrogenation reduction on the compound as shown in formula (I) in a solvent in the presence of a catalyst formed by a ligand, an iridium salt and an inorganic salt to form a compound as shown in formula (II), wherein the reaction formula is shown below. The catalyst used in an asymmetric catalytic hydrogenation synthesis method of the present invention is low in cost, the raw materials are completely converted, the ee value of the obtained target product can reach 99%, and thus the asymmetric catalytic hydrogenation synthesis method is suitable for industrial production.