CAS: 83928-76-1; 4,4-Dimethyl-1-(4-(4-(Pyrimidin-2-yl)Piperazin-1-yl)Butyl)Piperidine-2,6-Dione
- 英文名称4,4-Dimethyl-1-(4-(4-(Pyrimidin-2-yl)Piperazin-1-yl)Butyl)Piperidine-2,6-Dione
- 中文名称吉哌隆
- IUPAC名称4,4-dimethyl-1-(4-(4-(pyrimidin-2-yl)piperazin-1-yl)butyl)piperidine-2,6-dione
- 其它别名Gepirone; 4,4-Dimethyl-1-(4-(4-(Pyrimidin-2-yl)Piperazin-1-yl)Butyl)Piperidine-2,6-Dione; 4,4-Dimethyl-1-[4-[4-(2-Pyrimidinyl)-1-Piperazinyl]Butyl]-2,6-Piperidinedione; 2,6-Piperidinedione, 4,4-Dimethyl-1-(4-(4-(2-Pyrimidinyl)-1-Piperazinyl)Butyl)-; Gepirona; Gepirona [spanish]; Gepirone [inn]
- CAS编号83928-76-1
- MFCD编号:MFCD00868196
- FDA UNII编号:JW5Y7B8Z18
- 分子式:C19H29N5O2分子量:359.47
- 产品CID: 1827594
- 同类组份化合物CAS83928-66-9 (HCl)83928-76-1 (free base)
- 产品分类有机原料 → 有机杂环化合物 → 二嗪烷类
物理性质
上下游产品
CAS号20980-22-7 1-(2-嘧啶基)哌嗪 | CAS号84951-42-8 1-(4-bromobutyl... | CAS号1123-40-6 3,3-二甲基谷酰胺 | CAS号81461-73-6 8-(2-Pyrimidiny... | CAS号110-52-1 1,4-二溴丁烷合成工艺路线路线简述
- 2265884-97-5 = 83928-76-1
反应条件:1.1 Catalysts: Cobalt Chloride (Cocl2) Solvents: Tetrahydrofuran; Rt; 2 H,Rt1.2 Reagents: Ammonium Chloride Solvents: Water; Rt
标题:Late Stage Functionalization Of Secondary Amines Via A Cobalt-Catalyzed Electrophilic Amination Of Organozinc Reagents
作者:Grassl,Simon; Et Al
参考文献:Organic Letters 日期:2019 卷标:21(2) 页码:494-497]
= 83928-76-1
反应条件:1.1 Reagents: Hydrogen Catalysts: Palladium,Carbon Solvents: Ethyl Acetate
标题:Palladium(0)-Catalyzed Synthesis Of Buspirone And Gepirone
作者:Kuo,David L.
参考文献:Heterocycles 日期:1993 卷标:36(7) 页码:1463-9]
110-52-1 + 1123-40-6 = 83928-76-1
反应条件:1.1 Reagents: Potassium Carbonate Solvents: Acetonitrile; 80 °C1.2 Solvents: Acetonitrile; 80 °C; 16 H,80 °C2.1 Reagents: Potassium Carbonate Catalysts: Potassium Iodide Solvents: Acetonitrile; 20 H,80 °C
标题:Improved Synthesis Method For Gepirone
作者:Ye,Guangming; Et Al
参考文献:Dier Junyi Daxue Xuebao 日期:2005 卷标:26(2) 页码:223-224]
= 83928-76-1
反应条件:1.1 Reagents: Magnesium,Lithium Chloride,Zinc Chloride Solvents: Tetrahydrofuran; Heated; Overnight,Rt2.1 Catalysts: Cobalt Chloride (Cocl2) Solvents: Tetrahydrofuran; Rt; 2 H,Rt2.2 Reagents: Ammonium Chloride Solvents: Water; Rt
标题:Late Stage Functionalization Of Secondary Amines Via A Cobalt-Catalyzed Electrophilic Amination Of Organozinc Reagents
作者:Grassl,Simon; Et Al
参考文献:Organic Letters 日期:2019 卷标:21(2) 页码:494-497]
2265884-74-8 + 98-88-4 = 83928-76-1
反应条件:1.1 Reagents: Triethylamine Catalysts: 4-(Dimethylamino)Pyridine Solvents: Dichloromethane; 1 H,0 °C1.2 Reagents: Ammonium Chloride Solvents: Water2.1 Catalysts: Cobalt Chloride (Cocl2) Solvents: Tetrahydrofuran; Rt; 2 H,Rt2.2 Reagents: Ammonium Chloride Solvents: Water; Rt
标题:Late Stage Functionalization Of Secondary Amines Via A Cobalt-Catalyzed Electrophilic Amination Of Organozinc Reagents
作者:Grassl,Simon; Et Al
参考文献:Organic Letters 日期:2019 卷标:21(2) 页码:494-497]
106-96-7 + 1123-40-6 = 83928-76-1
反应条件:1.1 Reagents: Sodium Hydride Solvents: Dimethylformamide1.2 -2.1 Reagents: Cuprous Chloride Solvents: Ethanol,Water3.1 Reagents: Hydrogen
标题:A General Synthetic Method Suitable For The Introduction Of Deuterium Or Tritium In Buspirone-Type Anxiolytic Agents
作者:Welch,Willard M.; Et Al
参考文献:Journal Of Labelled Compounds And Radiopharmaceuticals 日期:1989 卷标:27(6) 页码:701-6]
20980-22-7 = 83928-76-1
反应条件:1.1 Solvents: Methanol; 12 H,55 °C2.1 Reagents: M-Chloroperbenzoic Acid Solvents: Dichloromethane; -78 °C; 1 H,-78 °C; > -78 °C; 12 H,Rt2.2 Reagents: Triethylamine Catalysts: 4-(Dimethylamino)Pyridine Solvents: Dichloromethane; 1 H,0 °C2.3 Reagents: Ammonium Chloride Solvents: Water3.1 Catalysts: Cobalt Chloride (Cocl2) Solvents: Tetrahydrofuran; Rt; 2 H,Rt3.2 Reagents: Ammonium Chloride Solvents: Water; Rt
标题:Late Stage Functionalization Of Secondary Amines Via A Cobalt-Catalyzed Electrophilic Amination Of Organozinc Reagents
作者:Grassl,Simon; Et Al
参考文献:Organic Letters 日期:2019 卷标:21(2) 页码:494-497]
81461-73-6 = 83928-76-1
反应条件:1.1 Solvents: Butyl Acetate
标题:Method Of Manufacturing Azapirones.
参考文献:European Patent Organization]
123319-76-6 + 84951-42-8 = 83928-76-1
反应条件:1.1 Reagents: Potassium Carbonate Catalysts: Potassium Iodide Solvents: Acetonitrile; 20 H,80 °C
标题:Improved Synthesis Method For Gepirone
作者:Ye,Guangming; Et Al
参考文献:Dier Junyi Daxue Xuebao 日期:2005 卷标:26(2) 页码:223-224]
= 83928-76-1
反应条件:1.1 Reagents: Hydrogen Catalysts: Palladium Solvents: Ethyl Acetate
标题:Process For The Preparation Of 2-(1-Piperazinyl)Pyrimidine Derivatives [e.G.,Gepirone]
参考文献:Switzerland]
= 83928-76-1
反应条件:1.1 Reagents: Hydrogen Catalysts: Palladium,Carbon Solvents: Ethyl Acetate
标题:Palladium(0)-Catalyzed Synthesis Of Buspirone And Gepirone
作者:Kuo,David L.
参考文献:Heterocycles 日期:1993 卷标:36(7) 页码:1463-9]
= 83928-76-1
反应条件:1.1 Reagents: Hydrogen
标题:A General Synthetic Method Suitable For The Introduction Of Deuterium Or Tritium In Buspirone-Type Anxiolytic Agents
作者:Welch,Willard M.; Et Al
参考文献:Journal Of Labelled Compounds And Radiopharmaceuticals 日期:1989 卷标:27(6) 页码:701-6]
20980-22-7 + 1123-40-6 = 83928-76-1
反应条件:1.1 Reagents: Potassium Carbonate Solvents: Dimethylformamide; 80 °C1.2 Reagents: 1,4-Butanediol,2,2-Dimethyl-,1,4-Dimethanesulfonate Solvents: Dimethylformamide; Rt1.3 Reagents: Potassium Carbonate Solvents: Dimethylformamide; 100 °C
标题:The Design And Preparation Of Metabolically Protected New Arylpiperazine 5-Ht1A Ligands
作者:Tandon,Manish; Et Al
参考文献:Bioorganic & Medicinal Chemistry Letters 日期:2004 卷标:14(7) 页码:1709-1712]
1722-12-9 = 83928-76-1
反应条件:1.1 Reagents: Sodium Carbonate Solvents: Water; 50 - 65 °C; 2 H,50 - 65 °C; 65 °C -> 35 °C1.2 Reagents: Hydrochloric Acid Solvents: Water; Acidified2.1 Reagents: Potassium Carbonate Catalysts: Potassium Iodide Solvents: Acetonitrile; 20 H,80 °C
标题:Improved Synthesis Method For Gepirone
作者:Ye,Guangming; Et Al
参考文献:Dier Junyi Daxue Xuebao 日期:2005 卷标:26(2) 页码:223-224]
20980-22-7 = 83928-76-1
反应条件:1.1 Reagents: Cuprous Chloride Solvents: Ethanol,Water2.1 Reagents: Hydrogen
标题:A General Synthetic Method Suitable For The Introduction Of Deuterium Or Tritium In Buspirone-Type Anxiolytic Agents
作者:Welch,Willard M.; Et Al
参考文献:Journal Of Labelled Compounds And Radiopharmaceuticals 日期:1989 卷标:27(6) 页码:701-6]
138274-09-6 + 98-88-4 = 83928-76-1
反应条件:1.1 Reagents: M-Chloroperbenzoic Acid Solvents: Dichloromethane; -78 °C; 1 H,-78 °C; > -78 °C; 12 H,Rt1.2 Reagents: Triethylamine Catalysts: 4-(Dimethylamino)Pyridine Solvents: Dichloromethane; 1 H,0 °C1.3 Reagents: Ammonium Chloride Solvents: Water2.1 Catalysts: Cobalt Chloride (Cocl2) Solvents: Tetrahydrofuran; Rt; 2 H,Rt2.2 Reagents: Ammonium Chloride Solvents: Water; Rt
标题:Late Stage Functionalization Of Secondary Amines Via A Cobalt-Catalyzed Electrophilic Amination Of Organozinc Reagents
作者:Grassl,Simon; Et Al
参考文献:Organic Letters 日期:2019 卷标:21(2) 页码:494-497]
20980-22-7 = 83928-76-1
反应条件:1.1 Catalysts: Tetrakis(Triphenylphosphine)Palladium Solvents: Tetrahydrofuran2.1 Reagents: Hydrogen Catalysts: Palladium,Carbon Solvents: Ethyl Acetate
标题:Palladium(0)-Catalyzed Synthesis Of Buspirone And Gepirone
作者:Kuo,David L.
参考文献:Heterocycles 日期:1993 卷标:36(7) 页码:1463-9]
20980-22-7 = 83928-76-1
反应条件:1.1 Reagents: Triethylamine Catalysts: Tetrakis(Triphenylphosphine)Palladium Solvents: Tetrahydrofuran2.1 Reagents: Hydrogen Catalysts: Palladium Solvents: Ethyl Acetate
标题:Process For The Preparation Of 2-(1-Piperazinyl)Pyrimidine Derivatives [e.G.,Gepirone]
参考文献:Switzerland
📜4,4-Dimethyl-1-<4-(4-Pyrimidin-2-Yl-Piperazin-1-yl)But-2-En-1-Yl>Piperidine-2,6-Dione置于palladium On Activated Charcoal 氢气体系中,用 乙酸乙酯 作为反应溶剂,以70%的收率获得产物吉哌隆
参考文献:Kuo,David L.,Heterocycles,1993,Vol. 36,# 7,P. 1463-1470
标题:Kuo,David L.,Heterocycles,1993,Vol. 36,# 7,P. 1463-1470
海关参考信息
- 2912110000-甲醛
2912120000-乙醛
2921211000-乙二胺
2924191000-二甲基甲酰胺 - 💡 提示：海关信息按照顺序优先匹配，如需确认的海关信息，请参考相关资料。
- 详情请参考：📖 海关编码查询和海关进出口税则
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-2022098170-A1
优先权日:2019-01-16
标 题 :Process for the synthesis of gepirone
发明人：COLOMBANO GIAMPIERO; BARBERO MAURO; GIOVENZANA GIOVANNI BATTISTA; ROLETTO JACOPO; PAISSONI PAOLO
权利人:PROCOS SPA
摘要:Disclosed is a process for the synthesis of gepirone of formula (I) from 8-(pyrimidin-2-yl)-5,8-diazaspiro[4,5]decan-5-ium bromide. The process according to the invention is economically efficient and easily industrially scalable.
专利号:US-2025283053-A1
优先权日:2022-04-20
标 题 :Enhanced cell-free bacteriophage synthesis by genetic modulation of bacterial transcription/translation machinery (txtl) machinery
发明人：BROOKS RANI
权利人:THE ADMINISTRATORS OF THE TULANE EDUCATIONAL FUND
摘要:The present disclosure relates to compositions including or obtained from genetically modified bacterial host cells (e.g., E. coli ) and methods for using the same for cell-free bacteriophage synthesis (CFBS). In particular, the present technology relates to genetically modified E. coli that overexpress one or more of translation initiation factor IF-3 (infC), OxyS and CyaR and/or repress RecC subunit exonuclease RecBCD, and methods for using the same to obtain improved CFBS yields.
专利号:US-7576211-B2
优先权日:2004-09-30
标题 :Synthesis of thienopyridinone compounds and related intermediates
发明人：DHANOA DALE S; BECKER OREN; NOIMAN SILVIA; CHEN DONGLI; MARANTZ YAEL; SHACHAM SHARON; HEIFETZ ALEXANDER; INBAL BOAZ; BAR-HAIM SHAY; MOHANTY PRADYUMNA; LOBERA MERCEDES; WU LAURENCE
权利人:EPIX DELAWARE INC
摘要:The invention relates to 5-HT receptor agonists and partial agonists. Novel thienopyridinone compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include Alzheimer's disease, cognition disorders, irritable bowel syndrome, nausea, emesis, vomiting, prokinesia, gastroesophageal reflux disease, nonulcer dyspepsia, depression, anxiety, urinary incontinence, migraine, arrhythmia, atrial fibrillation, ischemic stroke, gastritis, gastric emptying disorders, feeding disorders, gastrointestinal disorders, constipation, erectile dysfunction, and respiratory depression. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.
专利号:US-7309799-B2
优先权日:2004-06-01
标 题:Methods for the synthesis of milnacipran and congeners thereof
发明人：BUCHWALD STEPHEN L; SWAGER TIMOTHY M; RARIY ROMAN V
权利人:COLLEGIUM PHARMACEUTICAL INC
摘要:One aspect of the present invention relates to methods for synthesizing milnacipran or congeners thereof. Another aspect of the present invention relates to asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof. The present invention also relates to methods for synthesizing intermediates useful in the non-asymmetric or asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof.
专利号:US-12195777-B2
优先权日:2018-02-02
标 题 :Polynucleotide synthesis method, kit and system
发明人：HERON ANDREW JOHN
权利人:OXFORD NANEPORE TECH PLC; OXFORD NANOPORE TECH PLC
摘要:The invention relates to new in vitro methods for synthesising a polymer, particularly a polynucleotide molecule, having a pre-defined sequence of units such as nucleotides. For synthesising a polynucleotide molecule the methods involve a process of extending a polynucleotide synthesis molecule with a transfer nucleotide. The methods additionally involve repeating the extension process multiple times to iteratively extend the polynucleotide molecule with multiple transfer nucleotides to generate a new polynucleotide molecule having a pre-defined nucleotide sequence. The invention also relates to in vitro methods of joining multiple synthetic polynucleotides following synthesis to form larger synthetic polynucleotides, as well as devices and systems for performing the extension, synthesis and assembly methods of the invention.
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主要参考文献
1: Bayes M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2005 May;27(4):265-84. Review. Hungarian. Review. Review.
12: Amsterdam JD. Gepirone, a selective serotonin (5HT1A) partial agonist in the treatment of major depression. Prog Neuropsychopharmacol Biol Psychiatry. 1992 May;16(3):271-80. Review.
合成参考文献
摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2025).
参考文献:10.1007/bf02246344
摘要:Joordens RJ, Hijzen TH, Peeters BW, Olivier B. Fear-potentiated startle response is remarkably similar in two laboratories. Psychopharmacology (Berl). 1996 Jul;126(2):104–9. doi: 10.1007/bf02246344.
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