CAS: 845614-11-1; (S)-(4-(3-Fluoro-5-(Trifluoromethyl)Pyridin-2-yl)Piperazin-1-yl)(5-(Methylsulfonyl)-2-((1,1,1-Trifluoropropan-2-yl)Oxy)Phenyl)Methanone

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CAS号845616-81-1 3-氟-5-三氟甲基吡啶-2-哌嗪 | CAS号845616-82-2 (S)-2-(1-Methyl...

合成工艺路线路线简述

  • 247569-56-8 + 3539-97-7 = 845614-11-1
    反应条件:1.1 Reagents: Potassium Carbonate Solvents: Dimethylacetamide; 2 H,150 °C; 150 °C -> Rt1.2 Reagents: Hydrochloric Acid Solvents: Water; Ph 2,Rt2.1 Reagents: Diisopropylethylamine,O-(Benzotriazol-1-Yl)-N,N,N′,N′-Tetramethyluronium Tetrafluoroborate Solvents: Dimethylformamide; Overnight,Rt
    标题:Selective Glyt1 Inhibitors: Discovery Of [4-(3-Fluoro-5-Trifluoromethylpyridin-2-Yl)Piperazin-1-Yl][5-Methanesulfonyl-2-((S)-2,2,2-Trifluoro-1-Methylethoxy)Phenyl]Methanone (Rg1678),A Promising Novel Medicine To Treat Schizophrenia
    作者:Pinard,Emmanuel; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:2010 卷标:53(12) 页码:4603-4614]

    845616-82-2 + 845616-81-1 = 845614-11-1
    反应条件:1.1 Reagents: Diisopropylethylamine,O-(Benzotriazol-1-Yl)-N,N,N′,N′-Tetramethyluronium Tetrafluoroborate Solvents: Dimethylformamide; Overnight,Rt
    标题:Selective Glyt1 Inhibitors: Discovery Of [4-(3-Fluoro-5-Trifluoromethylpyridin-2-Yl)Piperazin-1-Yl][5-Methanesulfonyl-2-((S)-2,2,2-Trifluoro-1-Methylethoxy)Phenyl]Methanone (Rg1678),A Promising Novel Medicine To Treat Schizophrenia
    作者:Pinard,Emmanuel; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:2010 卷标:53(12) 页码:4603-4614]

    57260-71-6 + 89402-42-6 = 845614-11-1
    反应条件:1.1 Reagents: Potassium Carbonate Solvents: Acetonitrile; 2 H,Reflux; Reflux -> Rt1.2 Reagents: Trifluoroacetic Acid Solvents: Dichloromethane; 16 H,Reflux; Reflux -> Rt1.3 Reagents: Sodium Hydroxide Solvents: Water; Basified,Rt2.1 Reagents: Diisopropylethylamine,O-(Benzotriazol-1-Yl)-N,N,N′,N′-Tetramethyluronium Tetrafluoroborate Solvents: Dimethylformamide; Overnight,Rt
    标题:Selective Glyt1 Inhibitors: Discovery Of [4-(3-Fluoro-5-Trifluoromethylpyridin-2-Yl)Piperazin-1-Yl][5-Methanesulfonyl-2-((S)-2,2,2-Trifluoro-1-Methylethoxy)Phenyl]Methanone (Rg1678),A Promising Novel Medicine To Treat Schizophrenia
    作者:Pinard,Emmanuel; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:2010 卷标:53(12) 页码:4603-4614]

    865663-98-5 = 845614-11-1
    反应条件:1.1 Reagents: Lithium Hydroxide Solvents: Tetrahydrofuran,Water; 1 H,Rt1.2 Reagents: Hydrochloric Acid Solvents: Water; Ph 2,Rt2.1 Reagents: Potassium Carbonate Solvents: Dimethylacetamide; 2 H,150 °C; 150 °C -> Rt2.2 Reagents: Hydrochloric Acid Solvents: Water; Ph 2,Rt3.1 Reagents: Diisopropylethylamine,O-(Benzotriazol-1-Yl)-N,N,N′,N′-Tetramethyluronium Tetrafluoroborate Solvents: Dimethylformamide; Overnight,Rt
    标题:Selective Glyt1 Inhibitors: Discovery Of [4-(3-Fluoro-5-Trifluoromethylpyridin-2-Yl)Piperazin-1-Yl][5-Methanesulfonyl-2-((S)-2,2,2-Trifluoro-1-Methylethoxy)Phenyl]Methanone (Rg1678),A Promising Novel Medicine To Treat Schizophrenia
    作者:Pinard,Emmanuel; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:2010 卷标:53(12) 页码:4603-4614
2,3-二氯-5-三氟甲基吡啶置于potassium Carbonate,Cesium Fluoride体系中,用 二甲基亚砜,乙腈 作为反应溶剂,化学反应 52.0H,反应生成 (S)-[4-(3-氟-5-三氟甲基吡啶-2-基)哌嗪-1-基][5-(甲磺酰基)-2-(2,2,2-三氟-1-甲基乙氧基)苯基]甲酮
参考文献:Bitoper Tin的合成方法及其中间体
标题:Bitoper Tin的合成方法及其中间体
摘要:本发明公开了一种bitopertin的新合成方法及其中间体,本发明中提供的合成bitopertin的方法以5‑甲磺酰基‑2‑[(1S)‑2,2,2‑三氟‑1‑甲基乙氧基]苯甲酸为原料,通过氯代,酰化,脱保护,缩合和重结晶连续多步操作得到bitopertin,各步中间体不需要进一步纯化,其总收率可达80%以上.

海关参考信息

专利信息


专利号:US-7812161-B2
优先权日:2007-03-05
标 题 :Synthesis of GlyT-1 inhibitors
发明人：PFLEGER CHRISTOPHE; WALDMEIER PIUS; WANG SHAONING
权利人:HOFFMANN LA ROCHE
摘要:The present invention relates to a process for preparation of a compound of formula I n nwhereinn Het, R 1 , R 2 , R 3 , and n are as defined herein and pharmaceutically acceptable acid addition salts thereof, which comprises reacting a compound of formula 21 with a compound of formula 8 to obtain a compound of formula 11 and coupling the compound of formula 11 in the presence of a coupling reagent or the corresponding acid halogenide with a compound of formula 15 to obtain a compound of formula I.

专利号:WO-2008107334-A2
优先权日:2007-03-05
标题:Process for the synthesis of glyt-1 inhibitors

专利号:WO-2024193321-A1
优先权日:2023-03-17
标 题 :Use of glyt1 inhibitor in treatment of organ fibrosis
发明人：LI WEIDONG; LI XUEMIN; QIU JIALI; YANG KE; FU YUN; LI SHEN
权利人:UNIV TIANJIN MEDICAL
摘要:Use of a GLYT1 inhibitor in the treatment of organ fibrosis, especially the use in the preparation of a drug for treating organ fibrosis. By taking GLYT1 as a target, a GLYT1 inhibitor is used to inhibit a glycine transporter GLYT1 to achieve the treatment of fibrotic organs. The drug containing the GLYT1 inhibitor is particularly suitable for the treatment of pulmonary fibrosis. By inhibiting the glycine transporter GLYT1 by means of the GLYT1 inhibitor, collagen synthesis is reduced, so that pulmonary fibrosis caused by bleomycin can be obviously improved, and the formed pulmonary fibrosis is also obviously improved; and by taking GLYT1 as the target, the solution has a small influence on other physiological functions.

专利号:AU-2008223915-A1
优先权日:2007-03-05
标题:Process for the synthesis of GLYT-1 inhibitors

专利号:US-9751877-B2
优先权日:2012-09-21
标题 :Substituted pyrido[1,2-a]pyrazines for the treatment of neurodegenerative and neurological disorders
发明人：PETTERSSON MARTIN YOUNGJIN; JOHNSON DOUGLAS SCOTT; SUBRAMANYAM CHAKRAPANI; O'DONNELL CHRISTOPHER JOHN; AM ENDE CHRISTOPHER WILLIAM; GREEN MICHAEL ERIC; PATEL NANDINI CHATURBHAI; STIFF CORY MICHAEL; TRAN TUAN PHONG; KAUFFMAN GREGORY WAYNE; STEPAN ANTONIA FRIEDERIKE; VERHOEST PATRICK ROBERT
权利人:PFIZER
摘要:Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

专利号:US-2008221327-A1
优先权日:2007-03-05
标题:Synthesis of glyt-1 inhibitors

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主要参考文献


1: Deiana S, Hauber W, Munster A, Sommer S, Ferger B, Marti A, Schmid B, Dorner- Ciossek C, Rosenbrock H. Pro-cognitive effects of the GlyT1 inhibitor Bitopertin in rodents. Eur J Pharmacol. 2022 Nov 15;935:175306. doi: 10.1016/j.ejphar.2022.175306. Epub 2022 Sep 30. 71(6):621-2. doi: 10.1001/jamapsychiatry.2014.257. 4(22):e130111. doi: 10.1172/jci.insight.130111.
4: Javitt DC. Bitopertin in schizophrenia: glass half full? Lancet Psychiatry. 2016 Dec;3(12):1092-1093. doi: 10.1016/S2215-0366(16)30354-6. Epub 2016 Nov 2. 37(4):447-451. doi: 10.1097/JCP.0000000000000722.
6: Frouni I, Bédard D, Bourgeois-Cayer É, Hamadjida A, Gaudette F, Beaudry F, Huot P. Pharmacokinetic profile of bitopertin, a selective GlyT1 inhibitor, in the rat. Naunyn Schmiedebergs Arch Pharmacol. 2023 May;396(5):1053-1060. doi: 10.1007/s00210-022-02378-1. Epub 2023 Jan 12. 82(1):8-16. doi: 10.1016/j.biopsych.2016.11.014. Epub 2016 Dec 15.

合成参考文献


参考文献:10.1208/s12248-021-00674-x
摘要:Emami Riedmaier A. Predicting Food Effects: Are We There Yet AAPS J. 2022 Jan 10;24(1):25. doi: 10.1208/s12248-021-00674-x.
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