CAS: 82752-99-6; 1-(3-(4-(3-Chlorophenyl)Piperazin-1-yl)Propyl)-3-Ethyl-4-(2-Phenoxyethyl)-1H-1,2,4-Triazol-5(4H)-One Hydrochloride

该化合物是一种主要用作抗抑郁剂的药物化合物,属于被称为血清素受体和重新摄取抑制剂的药物类别. 内fazodone 的化学结构具有一种复杂的安排,其中包括苯基子子松,有助于其药理活动. 作为盐酸盐,它通常被作为白色的脱白晶粉呈色,在水中可溶解,在标准条件下具有中等稳定性. Nefazodone通过调节大脑中的血清素水平,从而缓解抑郁和焦虑症状.众所周知,它与其他抗抑郁剂相比具有相对有利的副作用,尽管它仍然可能造成一些病人的挥发性,眩晕和潜在的肝脏毒性.由于它独特的作用机制,当其他抗抑郁剂不起作用或不耐受力不力时,Nefazodone有时会被处死.但是,由于对肝脏安全以及新抗抑郁剂的可获性有了改善,其使用近年来有所下降.

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CAS号95885-13-5 5-乙基-4-(2-苯氧基乙基... | CAS号52605-52-4 1-(3-氯苯基)-4-(3-...

合成工艺路线路线简述

  • 95885-13-5 + 52605-52-4 = 82752-99-6
    反应条件:1.1 Reagents: Sodium Hydroxide Catalysts: Sodium Iodide Solvents: Isopropanol; 8 H,Reflux1.2 Reagents: Hydrochloric Acid Solvents: Water; Acidified
    标题:Improved Synthesis Of Nefazodone From Phenol
    作者:Li,Aijun; Et Al
    参考文献:Transactions Of Tianjin University 日期:2006 卷标:12(4) 页码:248-251]

    39577-43-0 + 95885-13-5 = 82752-99-6
    反应条件:1.1 Reagents: Sodium Hydroxide Solvents: Isopropanol,Water; 8 H,Reflux1.2 Reagents: Hydrochloric Acid Solvents: Ethanol; Ph 4
    标题:Synthesis Of 2-[3-[4-(3-Chlorophenyl)-1-Piperazinyl]Propyl]-5-Ethyl-2,4-Dihydro-4-(2-Phenoxyethyl)-3H-1,2,4-Triazol-3-One Hydrochloride (Nefazodone Hydrochloride)
    作者:Dong,Xinrong; Et Al
    参考文献:Huaxue Yanjiu 日期:2006 卷标:17(4) 页码:48-50]

    = 82752-99-6
    反应条件:1.1 Reagents: Sodium Hydroxide Solvents: Acetone,Water; 0 °C; 2 H,0 °C; 24 H,Rt2.1 Reagents: Sodium Hydroxide Solvents: Isopropanol,Water; 8 H,Reflux2.2 Reagents: Hydrochloric Acid Solvents: Ethanol; Ph 4
    标题:Synthesis Of 2-[3-[4-(3-Chlorophenyl)-1-Piperazinyl]Propyl]-5-Ethyl-2,4-Dihydro-4-(2-Phenoxyethyl)-3H-1,2,4-Triazol-3-One Hydrochloride (Nefazodone Hydrochloride)
    作者:Dong,Xinrong; Et Al
    参考文献:Huaxue Yanjiu 日期:2006 卷标:17(4) 页码:48-50]

    5818-15-5 + 17959-63-6 = 82752-99-6
    反应条件:1.1 -2.1 Reagents: Sodium Hydroxide Solvents: Isopropanol,Water; 8 H,Reflux2.2 Reagents: Hydrochloric Acid Solvents: Ethanol; Ph 4
    标题:Synthesis Of 2-[3-[4-(3-Chlorophenyl)-1-Piperazinyl]Propyl]-5-Ethyl-2,4-Dihydro-4-(2-Phenoxyethyl)-3H-1,2,4-Triazol-3-One Hydrochloride (Nefazodone Hydrochloride)
    作者:Dong,Xinrong; Et Al
    参考文献:Huaxue Yanjiu 日期:2006 卷标:17(4) 页码:48-50]

    = 82752-99-6
    反应条件:1.1 Reagents: Sodium Hydroxide Solvents: Methanol; 2 H,Rt; 15 H,Reflux2.1 Reagents: Sodium Iodide Solvents: Acetone; 15 H,Reflux2.2 Reagents: Ammonia Solvents: Methanol; 6 H,80 °C2.3 Reagents: Hydrochloric Acid Solvents: Methanol3.1 Reagents: Triethylamine Solvents: Chloroform; 2 H,Rt4.1 Reagents: Sodium Ethoxide Solvents: Xylene; 5 H,Reflux4.2 Reagents: Hydrochloric Acid Solvents: Water; Ph 45.1 Reagents: Sodium Hydroxide Catalysts: Sodium Iodide Solvents: Isopropanol; 8 H,Reflux5.2 Reagents: Hydrochloric Acid Solvents: Water; Acidified
    标题:Improved Synthesis Of Nefazodone From Phenol
    作者:Li,Aijun; Et Al
    参考文献:Transactions Of Tianjin University 日期:2006 卷标:12(4) 页码:248-251]

    95885-13-5 + 52605-52-4 = 82752-99-6
    反应条件:1.1 Reagents: Sodium Hydroxide Solvents: Isopropanol,Water; 2 H,Reflux1.2 Reagents: Hydrochloric Acid Solvents: Ethanol,Water; 1 H,Rt
    标题:Synthesis Of Nefazodone Hydrochloride
    作者:Guo,Baishu; Et Al
    参考文献:Zhongguo Yiyao Gongye Zazhi 日期:2003 卷标:34(6) 页码:265-266]

    5818-15-5 + 17959-63-6 = 82752-99-6
    反应条件:1.1 Reagents: Sodium Ethoxide Solvents: Xylene; 5 H,Reflux1.2 Reagents: Hydrochloric Acid Solvents: Water; Ph 42.1 Reagents: Sodium Hydroxide Catalysts: Sodium Iodide Solvents: Isopropanol; 8 H,Reflux2.2 Reagents: Hydrochloric Acid Solvents: Water; Acidified
    标题:Improved Synthesis Of Nefazodone From Phenol
    作者:Li,Aijun; Et Al
    参考文献:Transactions Of Tianjin University 日期:2006 卷标:12(4) 页码:248-251]

    95885-12-4 = 82752-99-6
    反应条件:1.1 Reagents: Potassium Hydroxide Solvents: Water; 40 Min,95 °C1.2 Reagents: Hydrochloric Acid Solvents: Water; 20 Min,0 °C; 1 H,Rt2.1 Reagents: Sodium Hydroxide Solvents: Isopropanol,Water; 2 H,Reflux2.2 Reagents: Hydrochloric Acid Solvents: Ethanol,Water; 1 H,Rt
    标题:Synthesis Of Nefazodone Hydrochloride
    作者:Guo,Baishu; Et Al
    参考文献:Zhongguo Yiyao Gongye Zazhi 日期:2003 卷标:34(6) 页码:265-266]

    5818-15-5 + 103965-96-4 = 82752-99-6
    反应条件:1.1 Reagents: Sodium Nitrite,Hydrochloric Acid Solvents: Toluene,Water; 0.5 H,0 °C1.2 Solvents: Toluene; 2 H,0 °C2.1 Reagents: Potassium Hydroxide Solvents: Water; 40 Min,95 °C2.2 Reagents: Hydrochloric Acid Solvents: Water; 20 Min,0 °C; 1 H,Rt3.1 Reagents: Sodium Hydroxide Solvents: Isopropanol,Water; 2 H,Reflux3.2 Reagents: Hydrochloric Acid Solvents: Ethanol,Water; 1 H,Rt
    标题:Synthesis Of Nefazodone Hydrochloride
    作者:Guo,Baishu; Et Al
    参考文献:Zhongguo Yiyao Gongye Zazhi 日期:2003 卷标:34(6) 页码:265-266]

    = 82752-99-6
    反应条件:1.1 Reagents: Hydrochloric Acid Solvents: Water; Rt; Rt -> Reflux; Reflux -> Rt1.2 Reagents: Sodium Hydroxide Solvents: Water; Ph 102.1 Reagents: Sodium Hydroxide Solvents: Acetone,Water; 0 °C; 2 H,0 °C; 24 H,Rt3.1 Reagents: Sodium Hydroxide Solvents: Isopropanol,Water; 8 H,Reflux3.2 Reagents: Hydrochloric Acid Solvents: Ethanol; Ph 4
    标题:Synthesis Of 2-[3-[4-(3-Chlorophenyl)-1-Piperazinyl]Propyl]-5-Ethyl-2,4-Dihydro-4-(2-Phenoxyethyl)-3H-1,2,4-Triazol-3-One Hydrochloride (Nefazodone Hydrochloride)
    作者:Dong,Xinrong; Et Al
    参考文献:Huaxue Yanjiu 日期:2006 卷标:17(4) 页码:48-50]

    17959-64-7 = 82752-99-6
    反应条件:1.1 Reagents: Triethylamine Solvents: Chloroform; 2 H,Rt2.1 Reagents: Sodium Ethoxide Solvents: Xylene; 5 H,Reflux2.2 Reagents: Hydrochloric Acid Solvents: Water; Ph 43.1 Reagents: Sodium Hydroxide Catalysts: Sodium Iodide Solvents: Isopropanol; 8 H,Reflux3.2 Reagents: Hydrochloric Acid Solvents: Water; Acidified
    标题:Improved Synthesis Of Nefazodone From Phenol
    作者:Li,Aijun; Et Al
    参考文献:Transactions Of Tianjin University 日期:2006 卷标:12(4) 页码:248-251]

    622-86-6 = 82752-99-6
    反应条件:1.1 Reagents: Sodium Iodide Solvents: Acetone; 15 H,Reflux1.2 Reagents: Ammonia Solvents: Methanol; 6 H,80 °C1.3 Reagents: Hydrochloric Acid Solvents: Methanol2.1 Reagents: Triethylamine Solvents: Chloroform; 2 H,Rt3.1 Reagents: Sodium Ethoxide Solvents: Xylene; 5 H,Reflux3.2 Reagents: Hydrochloric Acid Solvents: Water; Ph 44.1 Reagents: Sodium Hydroxide Catalysts: Sodium Iodide Solvents: Isopropanol; 8 H,Reflux4.2 Reagents: Hydrochloric Acid Solvents: Water; Acidified
    标题:Improved Synthesis Of Nefazodone From Phenol
    作者:Li,Aijun; Et Al
    参考文献:Transactions Of Tianjin University 日期:2006 卷标:12(4) 页码:248-251]

    7497-89-4 = 82752-99-6
    反应条件:1.1 Reagents: Hydrazine; 0.5 H,Rt; 18 H,40 - 50 °C2.1 Reagents: Sodium Nitrite,Hydrochloric Acid Solvents: Toluene,Water; 0.5 H,0 °C2.2 Solvents: Toluene; 2 H,0 °C3.1 Reagents: Potassium Hydroxide Solvents: Water; 40 Min,95 °C3.2 Reagents: Hydrochloric Acid Solvents: Water; 20 Min,0 °C; 1 H,Rt4.1 Reagents: Sodium Hydroxide Solvents: Isopropanol,Water; 2 H,Reflux4.2 Reagents: Hydrochloric Acid Solvents: Ethanol,Water; 1 H,Rt
    标题:Synthesis Of Nefazodone Hydrochloride
    作者:Guo,Baishu; Et Al
    参考文献:Zhongguo Yiyao Gongye Zazhi 日期:2003 卷标:34(6) 页码:265-266]

    = 82752-99-6
    反应条件:1.1 Reagents: Sodium; 40 H,95 - 110 °C2.1 Reagents: Hydrazine; 0.5 H,Rt; 18 H,40 - 50 °C3.1 Reagents: Sodium Nitrite,Hydrochloric Acid Solvents: Toluene,Water; 0.5 H,0 °C3.2 Solvents: Toluene; 2 H,0 °C4.1 Reagents: Potassium Hydroxide Solvents: Water; 40 Min,95 °C4.2 Reagents: Hydrochloric Acid Solvents: Water; 20 Min,0 °C; 1 H,Rt5.1 Reagents: Sodium Hydroxide Solvents: Isopropanol,Water; 2 H,Reflux5.2 Reagents: Hydrochloric Acid Solvents: Ethanol,Water; 1 H,Rt
    标题:Synthesis Of Nefazodone Hydrochloride
    作者:Guo,Baishu; Et Al
    参考文献:Zhongguo Yiyao Gongye Zazhi 日期:2003 卷标:34(6) 页码:265-266
📜5-乙基-4-(2-苯氧基乙基)-2H-1,2,4-三氮唑-3(4H)-酮,1-(3-氯苯基)-4-(3-氯丙基)哌嗪盐酸盐置于盐酸,Sodium Hydroxide体系中,用 二氯甲烷,异丙醇 作为反应溶剂,以62.5%的收率获得产物萘法唑酮盐酸盐
参考文献:1,2,4-Triazol-3-One Antidepressants
标题:1,2,4-Triazol-3-One Antidepressants
摘要:具有抗抑郁特性的苯氧烷基取代的1,2,4-三唑酮的典型代表是2-[3-[4-(3-氯苯基)-1-哌嗪基]丙基]-5-乙基-4-(2-苯氧乙基)-2H-1,2,4-三唑-3(4H)-酮.

海关参考信息

专利信息


专利号:US-2003083352-A1
优先权日:2000-07-31
标 题 :Synthesis of imidazole intermediates
发明人：HELAL CHRISTOPHER J
权利人:PFIZER
摘要:The invention provides a method for synthesis of compounds of formula n n n wherein R 1 and R 19 are as defined. Compounds of formula 12 are useful as intermediates for synthesizing compounds having pharmacological activity inhibiting cdk5, cdk2, and GSK-3.

专利号:US-2006030625-A1
优先权日:2004-08-06
标 题 :Dietary neurotransmitter precursors for balanced synthesis of neurotransmitters
发明人：HART CHERYLE RAM; GROSSMAN RONALD S; RAM HERBERT
权利人:HART CHERYLE RAM; GROSSMAN RONALD S; RAM HERBERT
摘要:Dietary supplements for treating a neurotransmitter deficiency include one or more precursors of the deficient neurotransmitter and a cofactor for activating in vivo enzymatic synthesis of the deficient neurotransmitter. The dietary supplements can also include an appropriate neurotransmitter, such as an amino acid. When administered through the oral mucosa, increases in levels of the deficient neurotransmitters and relief from deficiency symptoms are obtained.

专利号:US-12295961-B2
优先权日:2009-12-31
标 题:Modulation of solubility, stability, absorption, metabolism, and pharmacokinetic profile of lipophilic drugs by sterols
发明人：DHINGRA OM
权利人:MARIUS PHARMACEUTICALS INC
摘要:A formulation for drug delivery, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of a lipophilic therapeutic agent by formulation with sterols and/or sterol esters, resulting in higher bioavailability of a therapeutic agent administered to a subject in need of such therapeutic agent. The formulation contains a therapeutic agent and a sterol or sterol ester, and can, optionally, further contain a solubilizer and/or an enhancing agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.

专利号:US-11617758-B2
优先权日:2009-12-31
标 题 :Emulsion formulations
发明人：DHINGRA OM; BERNSTEIN JAMES S
权利人:MARIUS PHARMACEUTICALS LLC
摘要:A SEDDS or SMEDDS or SNEDDS formulation for drug delivery of a lipophilic therapeutic agent, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of the therapeutic agent by formulation with a lipophilic surfactant, a hydrophilic surfactant, one or more solubilizers and, optionally, digestible oils, resulting in higher bioavailability of the therapeutic agent administered to a subject in need of such therapeutic agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.

专利号:US-2013303495-A1
优先权日:2009-12-31
标题:Emulsion formulations
发明人：DHINGRA OM; BERNSTEIN JAMES S
权利人:SOV THERAPEUTICS; DIFFERENTIAL DRUG DEV ASSOCIATES LLC
摘要:A SEDDS or SMEDDS or SNEDDS formulation for drug delivery of a lipophilic therapeutic agent, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of the therapeutic agent by formulation with a lipophilic surfactant, a hydrophilic surfactant, one or more solubilizers and, optionally, digestible oils, resulting in higher bioavailability of the therapeutic agent administered to a subject in need of such therapeutic agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.

专利号:EP-3103803-B1
优先权日:2008-10-27
标 题 :Intermediates for the synthesis of mtor kinase inhibitors

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主要参考文献


1: Owens MJ, Ieni JR, Knight DL, Winders K, Nemeroff CB. The serotonergic antidepressant nefazodone inhibits the serotonin transporter: in vivo and ex vivo studies. Life Sci. 1995;57(24):PL373-80.

合成参考文献


参考文献:10.2165/11319380-000000000-00000
摘要:Chatzizisis YS, Koskinas KC, Misirli G, Vaklavas C, Hatzitolios A, Giannoglou GD. Risk factors and drug interactions predisposing to statin-induced myopathy: implications for risk assessment, prevention and treatment. Drug Saf. 2010 Mar 01;33(3):171–87. doi: 10.2165/11319380-000000000-00000.
参考文献:10.1155/2011/893905
摘要:Ishizaki J, Mimura M. Dysthymia and Apathy: Diagnosis and Treatment. Depression Research and Treatment. 2011;2011():1–7. doi: 10.1155/2011/893905.
参考文献:10.2165/11592070-000000000-00000
摘要:Watkins CC, Pieper AA, Treisman GJ. Safety considerations in drug treatment of depression in HIV-positive patients: an updated review. Drug Saf. 2011 Aug 01;34(8):623–39. doi: 10.2165/11592070-000000000-00000.
参考文献:10.1007/s10549-005-9056-0
摘要:Chien C, Li CI, Heckbert SR, Malone KE, Boudreau DM, Daling JR. Antidepressant use and breast cancer risk. Breast Cancer Research and Treatment. 2005 Dec 02;95(2):131–40. doi: 10.1007/s10549-005-9056-0.
参考文献:10.1007/s00535-005-1687-8
摘要:Hojo M, Miwa H, Yokoyama T, Ohkusa T, Nagahara A, Kawabe M, Asaoka D, Izumi Y, Sato N. Treatment of functional dyspepsia with antianxiety or antidepressive agents: systematic review. J Gastroenterol. 2005 Nov;40(11):1036–42. doi: 10.1007/s00535-005-1687-8.
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