📜(Z)-(1-(4-(2-(Benzyloxy)Ethoxy)Phenyl)-4-Chlorobut-1-Ene-1,2-Diyl)Dibenzene置于钯 氢气,钯,乙醇,水体系中,用 乙酸乙酯,乙醇 用作溶剂,化学反应生成欧司哌米 参考文献:Triphenylethylenes For The Prevention And Treatment Of Osteoporosis 标题:Triphenylethylenes For The Prevention And Treatment Of Osteoporosis 摘要:具有公式(i)的化合物,其中r.Sub.1和r.Sub.2独立地为h或oh,对于骨质疏松症的治疗和预防是有用的.公式(i)的化合物不具有明显的抗雌激素和雌激素活性.##str1##
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-12043612-B2 优先权日:2020-05-09 标 题 :Methods of manufacturing a bifunctional compound, ultrapure forms of the bifunctional compound, and dosage forms comprising the same 发明人:ALLAN LAURA E N; CHEN CHUNGPIN HERMAN; DONG HANQING; GROSSO JOHN A; HASKELL III ROYAL J; LLOYD RHYS; REECE HAYLEY 权利人:ARVINAS OPERATIONS INC 摘要:The present disclosure relates to ultra-pure forms, polymorphs, amorphous forms, and formulations of N-[(1r,4r)-4-(3-chloro-4-cyanophenoxy)cyclohexyl]-6-[4-({4-[2-(2,6-dioxopiperidin-3-yl)-6-fluoro-1,3-dioxo-2,3-dihydro-1H-isoindol-5-yl]piperazin-1-yl}methyl)piperidin-1-yl]pyridazine-3-carboxamide, referred to herein as Compound A:The present disclosure also relates methods of manufacturing and purifying the same, as well as intermediates useful in the synthesis of Compound A. The ultra-pure forms, polymorphs, amorphous forms, and formulations of Compound A can be used as therapeutic agents for the treatment of various diseases and conditions such as cancer.
专利号:US-9975832-B2 优先权日:2014-12-29 标题:Process for the preparation of ospemifene and fispemifene 发明人:CRISTIANO TANIA; ALPEGIANI MARCO 权利人:OLON SPA 摘要:Disclosed is a process for the synthesis of the active ingredients ospemifene and fispemifene which comprises reacting phenol 4 with an alkylating agent X—CH 2 CH 2 —Y of formula 7, wherein X is a leaving group and Y is the —(OCH 2 CH 2 ) n OH group wherein n is zero or 1; or X and Y, taken together, represent an oxygen atom; to give ospemifene or fispemifene of formula 8.
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: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:JP-7273802-B2 优先权日:2017-08-28 标题 :Asymmetric Synthesis of Compounds and Use in Disease Treatment
1: Di Carlo C, Cagnacci A, Murina F, Maffei S, Becorpi A, Lello S. Ospemifene and vulvovaginal atrophy: an update of the clinical profile for post-menopausal women. Expert Opin Pharmacother. 2024 Aug 12. doi: 10.1080/14656566.2024.2391009. Epub ahead of print. 16:1049-1053. doi: 10.2147/IJWH.S431520. 3: Meriggiola MC, Villa P, Maffei S, Becorpi A, Di Paolantonio T, Nicolucci A, Salvatore S, Nappi RE; PEONY Study Group. Vulvovaginal atrophy in women with and without a history of breast cancer: Baseline data from the PatiEnt satisfactiON studY (PEONY) in Italy. Maturitas. 2024 May;183:107950. doi: 10.1016/j.maturitas.2024.107950. Epub 2024 Mar 5. 66(1697):33-38. doi: 10.58347/tml.2024.1697a. 15(11):e49079. doi: 10.7759/cureus.49079.
合成参考文献
摘要:S109 | PARCEDC | List of 7074 potential endocrine disrupting compounds (EDCs) by PARC T4.2 | DOI:10.5281/zenodo.10944198