合成目标产物 Enzalutamide 主要起始原料 N-[3-Fluoro-4-[(Methylamino)Carbonyl]Phenyl]-2-Methylalanine And 4-Isothiocyanato-2-(Trifluoromethyl)Benzonitrile
1802242-43-8 = 915087-33-1 反应条件:1.1 Solvents: Tetrahydrofuran,Water; 40 Min,-10 °C; -10 °C -> 3 °C; 22 H,-8 °C1.2 Solvents: Ethanol 标题:An Improved And Practical Route For The Synthesis Of Enzalutamide And Potential Impurities Study 作者:Zhou,Ai-Nan; Et Al 参考文献:Chinese Chemical Letters 日期:2017 卷标:28(2) 页码:426-430
恩杂鲁胺杂质19 以4的收率获得产物4-[3-[4-氰基-3-(三氟甲基)苯基]-5,5-二甲基-4-氧代-2-硫酮-1-咪唑烷基]-2-氟-N-甲基苯甲酰胺 参考文献:Processes For The Synthesis Of Diarylthiohydantoin And Diarylhydantoin Compounds 标题:Processes For The Synthesis Of Diarylthiohydantoin And Diarylhydantoin Compounds 摘要:提供合成二芳基硫代异嘌呤和二芳基异嘌呤化合物的过程.含有这些化合物的药物产品在治疗前列腺癌方面具有特殊用途,包括去势抵抗性前列腺癌和/或激素敏感性前列腺癌.
专利号:US-9174943-B2 优先权日:2010-02-24 标 题 :Processes for the synthesis of diarylthiohydantoin and diarylhydantoin compounds 发明人:JAIN RAJENDRA PARASMAL; ANGELAUD REMY; THOMPSON ANDREW; LAMBERSON CAROL; GREENFIELD SCOTT 权利人:JAIN RAJENDRA PARASMAL; ANGELAUD REMY; THOMPSON ANDREW; LAMBERSON CAROL; GREENFIELD SCOTT; MEDIVATION PROSTATE THERAPEUTICS INC 摘要:Processes are provided for the synthesis of diarylthiohydantoin and diarylhydantoin compounds. Medicinal products containing the same find particular use in treating prostate cancer, including castration-resistant prostate cancer and/or hormone-sensitive prostate cancer.
专利号:US-11708381-B2 优先权日:2016-11-25 标题:Inhibitors of androgen receptor signaling 发明人:WANG GUANGDI; LIU JIAWANG; ZHENG SHILONG; GUO SHANCHUN 权利人:XAVIER UNIV OF LOUISIANA 摘要:The present disclosure relates to androgen receptor signaling inhibitors and the synthesis of the same. Further, the present disclosure teaches the utilization of the androgen receptor signaling inhibitors in a treatment for proliferative diseases, including cancer, particularly prostate cancer, and especially castration-resistant prostate cancer.
专利号:US-10626091-B2 优先权日:2014-10-01 标 题 :Process for the preparation of enzalutamide 发明人:CHIVUKULA KAMESWAR RAO; KARUTURI VEERA VENKATESWARA RAO; BENDA SRINIVAS; ANKE RAMACHANDRA; GAJULA DHARMAPURI; MOTURU VENKATA RAMA KRISHNA MURTHY; INDUKURI VENKATA SUNIL KUMAR; GORANTLA SEETA RAMA ANJANEYULU; CHAVA SATYANARAYANA 权利人:LAURUS LABS LTD 摘要:The present invention relates to an improved process for the preparation of enzalutamide by conventional synthesis, which avoids utilization of microwave irradiation and noxious reagents. The present invention also relates to an improved process for preparation of 4-isothiocyanato-2-(trifluoromethyl) benzonitrile, which is an intermediate in the synthesis of Enzalutamide.
专利号:US-2017190670-A1 优先权日:2014-07-11 标题:Improved process for the preparation of enzalutamide 发明人:HIRPARA SANJAY; SHRAWAT VIMAL KUMAR; POTHURAJU RAJU; TRIPATHI CHANDRESH KUMAR; AKSHAYKANT CHATURVEDI 权利人:SHILPA MEDICARE LTD 摘要:The present application relates to an improved process for preparation of Enzalutamide (I). n n n n n n n n n n The present application also relates to an improved process for the preparation of substantially pure Enzalutamide (I) having purity of greater than 99.5%. n The present application also relates to a novel process for the preparation of Enzalutamide intermediate useful in the industrially viable synthesis of Enzalutamide.
专利号:US-2022118094-A1 优先权日:2019-02-21 标题:Synthesis of biomimetic cell wall structure 发明人:WANG YONG; SHI PENG 权利人:PENN STATE RES FOUND 摘要:The present invention relates generally to methods of generating a biomimetic cell wall (BCW) on a target surface, compositions comprising the BCW, and methods of use of the compositions, including biomedical applications of the BCW coated compositions.
专利号:US-2025268920-A1 优先权日:2022-04-20 标 题:Use of androgen receptor-mediated mechanisms in the treatment of acute myeloid leukemia 发明人:QIAN FENGHUA; PRABHU KUMBLE SANDEEP; PAULSON ROBERT F 权利人:PENN STATE RES FOUND 摘要:Provided is a method for treating a blood cancer in an individual in need thereof by administrating to the individual an agent that inhibits activity or expression of one or more enzymes that participate in synthesis of either or both dihydrotestosterone (DHT) or androgen receptor (AR), or an antagonist AR, or a combination of an agent and the antagonist. The methods are shown in connection with acute myeloid leukemia (AML).
1: Gardner EJ, Ponnusamy S, Adelaiye-Ogala R. Coactivator networks orchestrating noncanonical AR programs in enzalutamide-resistant CRPC. Front Oncol. 2026 Jan 12;15:1748527. doi: 10.3389/fonc.2025.1748527. 2: Shore ND, Freedland SJ, Horvath LG, O'Sullivan JM, De Giorgi U, Ray EC, Ross AE, Tang Y, Russell D, Iwata KK, Rosales M, Ganguli A, Tombal B. Strategies to Mitigate Breast-related Adverse Events in Patients with High-risk Biochemically Recurrent Prostate Cancer Receiving Enzalutamide Monotherapy: Perspectives and Challenges. Eur Urol Focus. 2026 Jan;12(1):131-143. doi: 10.1016/j.euf.2025.11.015. Epub 2025 Dec 18. 2025 Nov. Report No.: PC0417. 58(1):189-199. doi: 10.1007/s11255-025-04663-3. Epub 2025 Jul 14. 22(5):605-616. doi: 10.1080/14796694.2025.2475730. Epub 2025 Jun 29. 6: Belabaci Z, Mose L, El-Taji O, Otmani Z, Hannouneh ZA, Mohamad I, Zilli T, Mohamad O, Pervez N, Arafat W, Vogl U, Shelan M. Safety and Efficacy of Reduced Dose of Enzalutamide in Patients with Castration-Resistant Prostate Cancer: A Systematic Review. Pharmaceuticals (Basel). 2025 May 16;18(5):732. doi: 10.3390/ph18050732.
合成参考文献
参考文献:10.1007/s00018-011-0766-7 摘要:Haile S, Sadar MD. Androgen receptor and its splice variants in prostate cancer. Cellular and Molecular Life Sciences. 2011 Jul 12;68(24):3971–81. doi: 10.1007/s00018-011-0766-7.