Methyl 3-[(3S,6S)-6-({(1R)-1-[3,5-Bis(Trifluoromethyl)Phenyl]Ethoxy}Methyl)-3-Nitro-6-Phenylpiperidin-3-Yl]Propanoate Methylsulfonate置于溶剂黄146,锌,盐酸,Sodium Carbonate体系中,用 水,甲苯 作为反应溶剂,化学反应生成 罗拉吡坦 参考文献:Hydrochloride Salts Of 8-[{1-(3,5-Bis-(Trifluoromethyl)Phenyl)-Ethoxy)-Methyl]-8-Phenyl-1,7-Diaza-Spiro[4.5]Decan-2-One And Preparation Process Therefor 标题:Hydrochloride Salts Of 8-[{1-(3,5-Bis-(Trifluoromethyl)Phenyl)-Ethoxy)-Methyl]-8-Phenyl-1,7-Diaza-Spiro[4.5]Decan-2-One And Preparation Process Therefor 摘要:本发明揭示了盐酸盐和对甲苯磺酸盐形式的(5S,8S)-8-[{(1R)-1-(3,5-双(三氟甲基)苯基)-乙氧基}-甲基]-8-苯基-1,7-二氮杂螺[4.5]癸烷-2-酮,由化学式i表示,并且揭示了制备这些盐的方法.
专利号:US-9260428-B2 优先权日:2007-03-22 标 题 :Process and intermediates for the synthesis of 8-[{1-(3,5-bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds 发明人:MERGELSBERG INGRID; SCHERER DOMINIK HERMANN; HUTTENLOCH MONIKA ERIKA; TSUI HON-CHUNG; PALIWAL SUNIL; SHIH NENG-YANG 权利人:OPKO HEALTH INC 摘要:This application discloses a process to synthesize 8-({1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy)-methyl]-8-pheny-1.7-diaza-spiro[4.5]decan-2-one comprising reacting a compound of the Formula 27a-sulfonate with zinc in the presence of acetic acid.
专利号:US-9822116-B2 优先权日:2008-09-05 标 题:Process and intermediates for the synthesis of 8-[{1-(3,5-bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds 发明人:WU GEORGE G; WERNE GERALD; FU XIAOYONG; ORR ROBERT K; CHEN FRANK XING; CUI JIAN; SPRAGUE VICTORIA M; ZHANG FUCHENG; XIE JI; ZENG LIANSHENG; CASTELLANOS LOUIS PETER; CHEN YUYIN; POIRIER MARC; MERGELSBERG INGRID 权利人:OPKO HEALTH INC 摘要:This application discloses a novel process to synthesize 8-[{1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds, which may be used, for example, as NK-1 inhibitor compounds in pharmaceutical preparations, intermediates useful in said process, and processes for preparing said intermediates; also disclosed is a process for removal of metals from N-heterocyclic carbine metal complexes.
专利号:US-2022118123-A1 优先权日:2019-02-22 标 题 :Combination of ar antagonists and targeted thorium conjugates 发明人:HAMMER STEFANIE; HAGEMANN URS BEAT; HAENDLER BERNARD; LEJEUNE PASCALE; ZITZMANN-KOLBE SABINE; SCHATZ CHRISTOPH; KARLSSON JENNY 权利人:BAYER AG; BAYER AS 摘要:The present invention covers combinations of at least two components, component A and component B, comprising component A being PSMA-TTC, and component B being an antiandrogen selected form AR antagonists such as from cyproterone acetate, bicalutamide, flutamide, nilutamide, enzalutamide, apalutamide, darolutamide or keto-darolutamide, or an AR degrader such as ARV-110, or an ARN-terminal domain binder such as EPI-506, or an antisense oligonucleotide that reduces AR expression such as EZN-4176 or AZD-5312, or an androgen synthesis inhibitor such as abiraterone, particularly abiraterone acetate, seviteronel, galeterone, orteronel or ketoconazole, or a dual AR antagonist and androgen synthesis inhibitor such as ODM-204. Another aspect of the present invention covers the use of such combinations as described herein for the preparation of a medicament for the treatment or prophylaxis of a disease, particularly for the treatment of a hyper-proliferative disease.
专利号:US-2025162973-A1 优先权日:2022-02-22 标题:Methods of synthesis and uses of agrimol compounds 发明人:CHE CHI MING; FU ZHIWEN; LEUNG YIU CHUNG GULICE 权利人:VERSITECH LTD; LABORATORY FOR SYNTHETIC CHEMISTRY AND CHEMICAL BIOLOGY LTD 摘要:Synthetic agrimol B and derivatives thereof (“compoundsâ€?) that have anticancer properties are disclosed. Methods for synthesizing the compounds with an overall yield ≥7% are disclosed. Pharmaceutical formulations in forms suitable for the delivery of the compounds to a subject in need thereof are disclosed. Methods of using the compounds for treating a cancer, reducing a cancer, or treating or ameliorating one or more symptoms associated with a cancer, such as non-small-cell lung cancer, in a subject are also disclosed. The methods include (i) administering to the subject the pharmaceutical formulation containing one or more compounds, for one or more times. The compounds can selectively kill cancer cells and/or cancer stem cells over noncancerous cells by inducing mitochondria dysfunction and/or inhibiting ER to Golgi trafficking in the cancer cells and/or cancer stem cells.
专利号:US-2014024834-A1 优先权日:2007-03-22 标题:Process and intermediates for the synthesis of 8-[-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds
专利号:US-10000493-B2 优先权日:2007-03-22 标 题:Process and intermediates for the synthesis of 8-[{1-(3,5-bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds
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合成参考文献
参考文献:10.1002/cpt.637 摘要:Wang X, Zhang ZY, Powers D, Wang J, Lu S, Kansra V. Rolapitant Absolute Bioavailability and PET Imaging Studies in Healthy Adult Volunteers. Clin Pharmacol Ther. 2017 Aug;102(2):332–9. doi: 10.1002/cpt.637.