2-Nitrocinnamic Acid置于钯体系中,用 乙醇 作为反应溶剂,化学反应生成 3,4-二氢-2(1H)-喹啉酮 参考文献:Carbostyril Derivatives As Combined Thromboxane Synthetase And 标题:Carbostyril Derivatives As Combined Thromboxane Synthetase And 摘要:该发明涉及一种抑制哺乳动物体内同时具有高血栓素水平或前列环素/血栓素水平失衡的疾病的方法,所使用的化合物具有以下结构式:X选自以下组合之一:和一个共价键,其中r.Sup.1为h,具有1-6个碳原子的烷基,可选择取代的苯基或可选择取代的苯基较低烷基,当r.Sup.2为h或oh时,或者r.Sup.1和r.Sup.2一起代表氧代,具有1-6个碳原子的烷基亚甲基或可选择取代的苄亚甲基;r.Sup.3为h或具有1-6个碳原子的烷基,R.Sup.4为h且r.Sup.3和r.Sup.4要么相对构型,要么相对构型,或者r.Sup.3和r.Sup.4一起代表一个共价键;n为0-3的整数;het为1-咪唑基或3-吡啶基;虚线代表可选择的共价键.
专利号:US-7759520-B2 优先权日:1996-11-27 标 题 :Synthesis of selective androgen receptor modulators 发明人:DALTON JAMES T; MILLER DUANE D; YIN DONGHUA; HE YALI 权利人:UNIV TENNESSEE RES FOUNDATION 摘要:The present invention relates to a synthetic process for the preparation of a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. The agents define a new subclass of compounds which are selective androgen receptor modulators (SARM) which are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia, osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and/or prevention of chronic muscular wasting; e) decreasing the incidence of, halting or causing a regression of prostate cancer; f) oral androgen relacement and/or other clinical therpauetic and/or diagnostic areas. The process of the present invention is suitable for large-scale preparation, since all of the steps give rise to highly pure compounds, thus avoiding complicated purification procedures which ultimately lower the yield. Thus the present invention provides methods for the synthesis of non-steroidal agonist compounds, that can be used for industrial large-scale synthesis, and that provide highly pure products in high yield.
专利号:US-3732204-A 优先权日:1967-07-17 标题 :Synthesis of acronycine and related compounds 发明人:BECK J 权利人:LILLY CO ELI 摘要:THE TOTAL SYNTHESIS OF ACRONYCINIC AND RELATED COMPOUNDS FROM READILY AVAILABLE STARTING MATERIALS IS DESCRIBED, AS ARE VARIOUS CLASSES OF INTRMEDIATES USEFUL IN THE SYNTHESIS.
专利号:US-6995284-B2 优先权日:2000-08-24 标题 :Synthesis of selective androgen receptor modulators 发明人:DALTON JAMES T; MILLER DUANE D; HE YALI; YIN DONGHUA 权利人:UNIV TENNESSEE RES FOUNDATION 摘要:The present invention relates to a synthetic process for the preparation of a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. The agents define a new subclass of compounds which are selective androgen receptor modulators (SARM) which are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia, osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and/or prevention of chronic muscular wasting; e) decreasing the incidence of, halting or causing a regression of prostate cancer; f) oral androgen relacement and/or other clinical therpauetic and/or diagnostic areas. The process of the present invention is suitable for large-scale preparation, since all of the steps give rise to highly pure compounds, thus avoiding complicated purification procedures which ultimately lower the yield. Thus the present invention provides methods for the synthesis of non-steroidal agonist compounds, that can be used for industrial large-scale synthesis, and that provide highly pure products in high yield.
专利号:US-3624087-A 优先权日:1967-07-17 标 题:Synthesis of acronycine and related compounds 发明人:BECK JAMES R 权利人:LILLY CO ELI 摘要:The total synthesis of acronycine and related compounds from readily available starting materials is described, as are various classes of intermediates useful in the synthesis.
专利号:US-12006301-B1 优先权日:2021-05-13 标题 :And synthesis of dual 5-HT1A and 5-HT7 receptor ligands 发明人:ABLORDEPPEY SETH Y 权利人:FLORIDA A&M UNIV 摘要:Novel dual 5-HT1A and 5-HT7 receptor ligands and methods of using the novel ligands to treat a neurological disorder are presented.
专利号:US-2024174698-A1 优先权日:2022-09-23 标题 :Modular synthesis of 1,2-azaborines via ring-opening bn-isostere benzannulation 发明人:DONG GUANGBIN; LYU HAIRONG; CHEN ZHIJIE; WU YIFEI; CHOI SHINYOUNG 权利人:UNIV CHICAGO 摘要:The present disclosure relates generally to 1,2-azaborines and methods of making the same.
1: Wang S, Liu H, Lei K, Li G, Li J, Wei Y, Wang X, Liu R. Synthesis of 3,4-dihydroquinolin-2(1H)-one derivatives with anticonvulsant activity and their binding to the GABAA receptor. Bioorg Chem. 2020 Oct;103:104182. doi: 10.1016/j.bioorg.2020.104182. Epub 2020 Aug 27. 206:112672. doi: 10.1016/j.ejmech.2020.112672. Epub 2020 Aug 6. 30(13):127223. doi: 10.1016/j.bmcl.2020.127223. Epub 2020 Apr 27. 35(1):1021-1026. doi: 10.1080/14756366.2020.1751620. 5: Ogino M, Fedorov Y, Adams DJ, Okada K, Ito N, Sugiyama M, Ogino T. Vesiculopolins, a New Class of Anti-Vesiculoviral Compounds, Inhibit Transcription Initiation of Vesiculoviruses. Viruses. 2019 Sep 14;11(9):856. doi: 10.3390/v11090856.
合成参考文献
摘要:Tang, X.; Shi, M., Science of Synthesis: Metal-Catalyzed Cyclization Reactions, (2016) 1, 221. 摘要:Zhou, M.; Qin, T., Science of Synthesis, (2020) , 517. 摘要:Cheng, Q.; Shen, X., Science of Synthesis: Knowledge Updates, (2025) 2. 摘要:Inagi, S.; Taniguchi, K.; Lam, K., Science of Synthesis: Modern Strategies in Organofluorine Chemistry, (2024) 2. 参考文献:10.1007/s00894-019-4091-7 摘要:Moreira CA, Custódio JMF, Vaz WF, D’Oliveira GDC, Noda Perez C, Napolitano HB. A comprehensive study on crystal structure of a novel sulfonamide-dihydroquinolinone through experimental and theoretical approaches. Journal of Molecular Modeling. 2019 Jun 29;25(7):205. doi: 10.1007/s00894-019-4091-7.