114812-34-9 + 32541-62-1 = 84225-95-6 反应条件:1.1 Reagents: Lithium Aluminum Hydride Solvents: Tetrahydrofuran1.2 Reagents: Triethylamine Solvents: Dichloromethane1.3 Reagents: Boron Tribromide 标题:N-Fluoroalkylated And N-Alkylated Analogs Of The Dopaminergic D-2 Receptor Antagonist Raclopride 作者:Lannoye,G. S.; Moerlein,Stephen M.; Parkinson,D.; Welch,M. J. 参考文献:Journal Of Medicinal Chemistry 日期:1990 卷标:33(9) 页码:2430-7]
84225-94-5 = 84225-95-6 反应条件:1.1 Reagents: Hydrochloric Acid,Boron Tribromide Solvents: Dichloromethane 标题:Synthesis Of [methoxy-3H]- And [methoxy-11C]-Labeled Raclopride. Specific Dopamine-D2 Receptor Ligands 作者:Ehrin,Erling; Gawell,Lars; Hoegberg,Thomas; De Paulis,Tomas; Stroem,Peter 参考文献:Journal Of Labelled Compounds And Radiopharmaceuticals 日期:1987 卷标:24(8) 页码:931-40
📜3,5-Dichloro-2,6-Dimethoxybenzoyl Chloride置于三溴化硼体系中,用 二氯甲烷 作为反应溶剂,化学反应生成 雷氯必利 参考文献:An Improved Synthesis Of Pet Dopamine D2 Receptors Radioligand [11C]Raclopride 标题:An Improved Synthesis Of Pet Dopamine D2 Receptors Radioligand [11C]Raclopride 摘要:An Improved Synthesis Of [c-11]Raclopride Is Reported. The Precursor Desmethyl-Raclopride Was Synthesized From 3,5-Dichloro-2,6-Dimethoxybenzoic Acid And (S)-(-)-2-Aminoethyl-1-Ethylpyrrolidine Via A Straightforward,Four-Step Synthetic Approach With 29% Overall Chemical Yield. [c-11]Raclopride Was Prepared By O-[c-11]Methylation Of The Precursor With [c-11]Methyl Triflate And Purification With A Semi-Preparative HPLC Method In 20-34% Radiochemical Yield,Based On [c-11]Methyl Bromide,Decay Corrected To End Of Bombardment (Eob). DOI:10.1081/scc-120034174
专利号:US-2022009919-A1 优先权日:2009-12-17 标题:Preparation of n-monofluoroalkyl compounds 发明人:WILLIAMS LORENZO; KEILEN GUNNAR; HAUGAN JARLE ANDRE 权利人:GE HEALTHCARE LTD 摘要:The present invention relates to an improved synthesis of N-monofluoroalkyl tropanes using fluoroalkyl iodide. The invention also provides the use of such method to prepare the non-radioactive tropane intermediate FP-CIT, and its subsequent conversion to the 123 I-labelled radiopharmaceutical DaTSCANâ„¢ ( 123 I-ioflupane). Also provided is the use of fluoroalkyl iodide in the alkylation method of the invention.
专利号:US-6749830-B2 优先权日:2001-01-31 标 题:Method for the synthesis of radiolabeled compounds 发明人:WILSON ALAN ALEXANDER; GARCIA ARMANDO FRANCISCO; JIN LI; HOULE SYLVAIN JOSEPH 权利人:CAMH 摘要:The present invention relates to a new method for radiolabeling chemical compounds. The new method attains the goals of simplicity, high radiochemical yields, speed, versatility, and automation. An HPLC injection loop on an HPLC injection valve is loaded with a solution of precursor and the radiolabeling reagent is passed through the loop. The contents of the loop are then quantitatively injected onto the HPLC column for purification. Radiochemical yields are equal to or superior to conventional solution methods in all cases, even though no heat need be applied. Since no vials, transfer lines, cooling, heating, or sealing valves are required, no transfer losses occur, yields are high, and clean-up is minimal. This “loop methodâ€? is ideal for the preparation of radiolabeled compounds, in particular those prepared from [ 11 C]-iodomethane.
专利号:US-6872716-B2 优先权日:2000-09-11 标题:Antipsychotic sulfonamide-heterocycles, and methods of use thereof 发明人:WU XINHE; AQUILA BRIAN M; SHAO LIMING; RADEKE HEIKE; CUNY GREGORY D; HAUSKE JAMES R; XIE ROGER L 权利人:SEPRACOR INC 摘要:One aspect of the present invention relates to heterocyclic compounds comprising a sulfonamide moiety. A second aspect of the present invention relates to the use of the heterocyclic compounds comprising a sulfonamide moiety to treat diseases, afflictions or maladies caused at least in part by abnormal activity of one or more GPCRs or ligand-gated ion channels. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds comprising a sulfonamide moiety, and the screening of those libraries for biological activity, e.g., in animal models of psychosis.
专利号:US-2002155063-A1 优先权日:2001-01-31 标 题 :Method for the synthesis of radiolabeled compounds
专利号:US-2007160574-A1 优先权日:2000-04-12 标题 :Design of CXC chemokine analogs for the treatment of human diseases 发明人:MERZOUK AHMED; SALARI HASSAN 权利人:MERZOUK AHMED; SALARI HASSAN 摘要:The present invention generally relates to the design, preparation, derivation, and use of mimetics of CXC chemokines (CXCL1-CXCL17) in the prevention, treatment, and ameliorization of a wide variety of diseases and disorders. Generally speaking, this invention is directed to the design, synthesis, and use of chemokine analogs which bind to CXC chemokine receptors CXCR1-CXCR7, such that the analogs can be designed to affect the activity of the receptor, either as an agonist or an antagonist. The analogs can be useful for treating a wide variety of diseases and disorders, and can also serve as an adjunct to the treatment of a variety of diseases and disorders.
专利号:EP-4630405-A1 优先权日:2022-12-06 标题 :Process for the synthesis of substituted tetrahydrofuran modulators of sodium channels
参考文献:10.1038/mp.2011.86 摘要:Wang GJ, Smith L, Volkow ND, Telang F, Logan J, Tomasi D, Wong CT, Hoffman W, Jayne M, Alia-Klein N, Thanos P, Fowler JS. Decreased dopamine activity predicts relapse in methamphetamine abusers. Mol Psychiatry. 2012 Sep;17(9):918–25. 参考文献:10.1016/j.neuropharm.2011.06.025 摘要:Orrú M, Quiroz C, Guitart X, Ferré S. Pharmacological evidence for different populations of postsynaptic adenosine A2A receptors in the rat striatum. Neuropharmacology. 2011 Oct;61(5-6):967–74. doi: 10.1016/j.neuropharm.2011.06.025. 参考文献:10.1007/s00415-011-6168-9 摘要:Kono S, Ouchi Y, Terada T, Suzuki M, Yagi S, Miyajima H. Combined FDG and raclopride PET study in a case of ALS with the R521C FUS gene mutation. J Neurol. 2012 Feb;259(2):367–9. doi: 10.1007/s00415-011-6168-9. 参考文献:10.1016/j.neuroimage.2011.07.002 摘要:Normandin MD, Schiffer WK, Morris ED. A linear model for estimation of neurotransmitter response profiles from dynamic PET data. NeuroImage. 2012 Feb;59(3):2689–99. doi: 10.1016/j.neuroimage.2011.07.002. 参考文献:10.1017/s146114571100109x 摘要:Sutton LP, Rushlow WJ. The dopamine D2 receptor regulates Akt and GSK-3 via Dvl-3. Int J Neuropsychopharmacol. 2012 Aug;15(7):965–79. doi: 10.1017/s146114571100109x.