CAS: 456-59-7; 3,3,5-Trimethylcyclohexyl 2-Hydroxy-2-Phenylacetate

该化合物是化学结构,包括环形环和酯功能组,有助于其药理特性.Cyclandelate通常被作为白色的脱白晶粉,在水中表现出低溶性,但在有机溶剂中表现出较高的溶性.其行动机制包括血管滑动肌肉放松,导致血液流动增加,特别是在极端地区.此外,对环状板进行了研究,以了解其潜在的...

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3,3,5-trimethylcyclohexanol MANDELIC ACID Benzoylformic acid 3,3,5-trimethylcyclohexyl 2-oxo-2-phenylacetate

合成工艺路线路线简述

  • 合成目标产物 Cyclandelate 主要起始原料 3,3,5-Trimethylcyclohexanol And Benzoylformic Acid
  • (文献来源)合成步骤主要原料 3,3,5-Trimethylcyclohexanol 和 Benzoylformic Acid
3,3,5-三甲基环己基2-氧亚基-2-苯基醋酸盐置于水,Sodium Acetate,双二苯基膦甲烷,Cobalt(II) Iodide,锌体系中,用 乙腈 作为反应溶剂,化学反应 12.0H,以91%的收率获得产物环扁桃酯
参考文献:以h2O为氢源的α-酮酸酯和n-环硫磺酰亚胺的钴催化转移加氢
标题:以h2O为氢源的α-酮酸酯和n-环硫磺酰亚胺的钴催化转移加氢
摘要:描述了一种以安全和环境友好的H2O作为氢源对各种α-酮酸酯和n-环磺酰亚胺的共催化有效转移加氢方法.该反应使用容易获得并且易于处理锌金属作为还原剂.有趣的是,催化体系不需要用于还原n-环磺酰亚胺的配体.
DOI:10.1002/adsc.201900636

海关参考信息

专利信息


专利号:US-5442065-A
优先权日:1993-09-09
标 题:Synthesis of tetrahydroquinoline enediyne core analogs of dynemicin
发明人:MAGNUS PHILIP D; ILIADIS THEODORE; EISENBEIS SHANE A; FAIRHURST ROBIN A
权利人:UNIV TEXAS
摘要:A process is described for the preparation of the core azobicyclo[7.3.1]tridecaenediyne moiety of the antitumor antibiotic dynemicin. The synthesis allows efficient production of the enediyne as a stable, compound in good yield from the adamantyl N-protected azabicyclo[7.3.1]tridecadiyne. The adamantyl protecting group is employed in the starting material, N-adamantyl dihydroquinoline or N-adamantyl 6-methoxy quinoline. Also disclosed are process for the synthesis of 3-hydroxy-6-methoxyquinoline and several N-substituted derivatives of azobicyclo[7.3.1]tridecaenediyne. Solid tumor and leukemia assays were performed on the analogs of dynemicin. The results suggest a method that these compounds will useful in treating certain types of leukemias and solid tumors. The disclosed synthesis provides a route to new dynemicin intermediates and analogs which will allow development of second and third generation dynemicins.

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-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-11858953-B2
优先权日:2018-04-04
标 题:Compositions and methods for synthesis of phosphorylated molecules
发明人:CHAPUT JOHN; LIAO JEN-YU; BALA SAIKAT
权利人:UNIV CALIFORNIA
摘要:The invention provides compositions and methods for synthesis of phosphorylated organic compounds, including nucleoside triphosphates.

专利号:US-2015336866-A1
优先权日:2013-01-01
标题:Synthesis of difluoromethyl ethers and sulfides
发明人:HARTWIG JOHN; FIER PATRICK
权利人:UNIV CALIFORNIA
摘要:The synthesis of difluoromethyl ethers and sulfides with a simple, non-ozone-depleting reagent is described. The difluoromethylation of phenols with this reagent occurs at room temperature within minutes with exceptional functional group tolerance. The mild conditions makes possible tandem processes for the conversion of aryl boronic acids, aryl halides and arenes to difluoromethyl ethers. Mechanistic studies support a reaction pathway involving nucleophilic attack of the phenolate to difluorocarbene.

专利号:US-11708341-B2
优先权日:2016-08-05
标题:Synthesis of (S)-2-amino-4-methyl-((R)-2-methyloxirane-2-yl)-pentan-1-one and pharmaceutically acceptable salts thereof
发明人:Beaver Matthew; CUI SHENG; SHI XIANGQING
权利人:AMGEN INC
摘要:The present invention provides new methods for preparing compound 5, and pharmaceutically acceptable salts thereof, of structure n nCompound 5, or a pharmaceutically acceptable salt thereof, is an important intermediate in the synthesis of carfilzomib. The invention further provides methods of making a useful manganese catalyst that may be used in the epoxidation step of the present invention.
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主要参考文献


1: Diener HC, Krupp P, Schmitt T, Steitz G, Milde K, Freytag S. Cyclandelate in the prophylaxis of migraine: a placebo-controlled study. Cephalalgia. 2001 Feb;21(1):66-70. German. Japanese.

合成参考文献


摘要:Drugs in Japan, 6(310), 1982
摘要:The Merck Index. 9th ed. Rahway, New Jersey: Merck & Co., Inc., 1976., p. 352
参考文献:10.1002/ana.410070421
摘要:van der Drift JH. Cyclandelate in diabetic radiculoneuropathy. Ann Neurol. 1980 Apr;7(4):388. doi: 10.1002/ana.410070421.
参考文献:10.1016/s1043-6618(05)80078-7
摘要:Dimpfel W, Wedekind W, Spüler M. Field potential analysis in the freely moving rat during the action of cyclandelate or flunarizine. Pharmacol Res. 1992 Apr;25(3):287–97. doi: 10.1016/s1043-6618(05)80078-7.
参考文献:10.2165/11534630-000000000-00000
摘要:Ruggiero C, Lattanzio F, Dell'Aquila G, Gasperini B, Cherubini A. Inappropriate drug prescriptions among older nursing home residents: the Italian perspective. Drugs Aging. 2009 Dec;26 Suppl 1():15–30. doi: 10.2165/11534630-000000000-00000.
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