61341-26-2 = 81452-54-2 反应条件:1.1 Solvents: Methanol; 4 H,Rt -> 45 °C 标题:Development Of Potential Manufacturing Routes For Substituted Thiophenes - Preparation Of Halogenated 2-Thiophenecarboxylic Acid Derivatives As Building Blocks For A New Family Of 2,6-Dihaloaryl 1,2,4-Triazole Insecticides 作者:Hull,John W. Jr.; Et Al 参考文献:Beilstein Journal Of Organic Chemistry 日期:2007 卷标:3]
26137-08-6 + 80-48-8 = 81452-54-2 反应条件:1.1 Reagents: Tetrabutylammonium Iodide,Zinc,Magnesium Chloride Catalysts: 4,4′-Dimethyl-2,2′-Bipyridine,Nickel Iodide (Nii2) Solvents: Dimethylacetamide; 12 H,Rt 标题:Nickel-Catalyzed Methylation Of Aryl Halides/tosylates With Methyl Tosylate 作者:Wang,Jiawang; Et Al 参考文献:Chemical Communications (Cambridge 日期:2017 卷标:53(73) 页码:10180-10183]
181226-89-1 + 80-48-8 = 81452-54-2 反应条件:1.1 Reagents: Tetrabutylammonium Iodide,Zinc,Magnesium Chloride Catalysts: Triphenylphosphine,Dichloro[1,2-Di(Methoxy-Ko)Ethane]Nickel Solvents: Dimethylacetamide; 12 H,25 °C 标题:Nickel-Catalyzed Methylation Of Aryl Halides/tosylates With Methyl Tosylate 作者:Wang,Jiawang; Et Al 参考文献:Chemical Communications (Cambridge 日期:2017 卷标:53(73) 页码:10180-10183]
14282-76-9 = 81452-54-2 反应条件:1.1 Reagents: Magnesium Solvents: Tetrahydrofuran; < 40 °C; 60 Min,25 °C1.2 0.1 H,25 °C; 4 H,25 °C1.3 Reagents: Hydrochloric Acid Solvents: Water; Rt 标题:Development Of Potential Manufacturing Routes For Substituted Thiophenes - Preparation Of Halogenated 2-Thiophenecarboxylic Acid Derivatives As Building Blocks For A New Family Of 2,6-Dihaloaryl 1,2,4-Triazole Insecticides 作者:Hull,John W. Jr.; Et Al 参考文献:Beilstein Journal Of Organic Chemistry 日期:2007 卷标:3]
16494-40-9 = 81452-54-2 反应条件:1.1 Reagents: Magnesium Solvents: Diethyl Ether 标题:A New Synthesis Of Benzo[b]Thiophenes And Benzo[c]Thiophenes By Annulation Of Disubstituted Thiophenes 作者:Terpstra,Jan W.; Et Al 参考文献:Journal Of Organic Chemistry 日期:1986 卷标:51(2) 页码:230-8]
13679-72-6 = 81452-54-2 反应条件:1.1 Catalysts: Sodium Hypobromite2.1 Solvents: Methanol 标题:Synthesis And Properties Of Methyl 3,4-Dihydro-4-Oxo-1H-2-Benzothiopyran-3-Carboxylate And Related Thiopyrano Compounds 作者:Scrowston,Richard M.; Et Al 参考文献:Journal Of The Chemical Society 日期:1976 卷标:(7) 页码:749-54]
23806-24-8 = 81452-54-2 反应条件:1.1 Reagents: Thionyl Chloride Solvents: Dimethylformamide,1,2-Dichloroethane; 2 H,Reflux2.1 Solvents: Methanol; 4 H,Rt -> 45 °C 标题:Development Of Potential Manufacturing Routes For Substituted Thiophenes - Preparation Of Halogenated 2-Thiophenecarboxylic Acid Derivatives As Building Blocks For A New Family Of 2,6-Dihaloaryl 1,2,4-Triazole Insecticides 作者:Hull,John W. Jr.; Et Al 参考文献:Beilstein Journal Of Organic Chemistry 日期:2007 卷标:3]
59201-85-3 + 62353-77-9 + 51202-29-0 = 81452-54-2 反应条件:1.1 Catalysts: Di-μ-Chlorobis(η3-2-Propenyl)Dipalladium Solvents: Dimethylformamide 标题:A Convenient Synthesis Of Substituted Heteroaromatic Compounds Via The Palladium-Catalyzed Cross-Coupling Reaction Of Organosilicon Compounds 作者:Hatanaka,Yasuo; Et Al 参考文献:Heterocycles 日期:1990 卷标:30(1) 页码:303-6]
5834-16-2 = 81452-54-2 反应条件:1.1 Reagents: Hydrogen Peroxide Catalysts: Perchloric Acid,Iron(3+) Salt,Hydrate Solvents: Methanol,Water; 4 H,0 °C; 1 H,0 °C; 0 °C -> Rt; 15 H,Rt 标题:Iron-Catalyzed One-Pot Oxidative Esterification Of Aldehydes 作者:Wu,Xiao-Feng; Et Al 参考文献:European Journal Of Organic Chemistry 日期:2009 卷标:(8) 页码:1144-1147]
= 81452-54-2 反应条件:1.1 Reagents: Oxygen Catalysts: Chloro(Triphenylphosphine)Gold,[1,1,1-Trifluoro-N-[(Trifluoromethyl)Sulfonyl-Ko]Methanesulfonamidato-Ko]Silver Solvents: Dichloromethane; 10 Min,1 Atm,Rt1.2 Reagents: Methanol,Oxygen Solvents: Dichloromethane; 24 H,1 Atm,25 °C 标题:Gold-Catalyzed Oxidative Cleavage Of Aryl-Substituted Alkynyl Ethers Using Molecular Oxygen. Simultaneous Degradation Of C-H And Single And Triple Carbon-Carbon Bonds Under Ambient Conditions 作者:Das,Arindam; Et Al 参考文献:Chemical Communications (Cambridge 日期:2009 卷标:(27) 页码:4046-4048]
5118-06-9 = 81452-54-2 反应条件:1.1 Reagents: Triethylamine Catalysts: 4-(Dimethylamino)Pyridine Solvents: Dichloromethane; 15 Min,0 °C; 0 °C -> Rt; 2 H,Rt2.1 Reagents: Tetrabutylammonium Iodide,Zinc,Magnesium Chloride Catalysts: Triphenylphosphine,Dichloro[1,2-Di(Methoxy-Ko)Ethane]Nickel Solvents: Dimethylacetamide; 12 H,25 °C 标题:Nickel-Catalyzed Methylation Of Aryl Halides/tosylates With Methyl Tosylate 作者:Wang,Jiawang; Et Al 参考文献:Chemical Communications (Cambridge 日期:2017 卷标:53(73) 页码:10180-10183]
= 81452-54-2 反应条件:1.1 Reagents: Acetic Anhydride,N-Bromosuccinimide Solvents: Acetic Acid; Rt -> 44 °C; 20 Min,Rt1.2 Reagents: Sodium Bisulfite Solvents: Water; 0 °C2.1 Reagents: Magnesium Solvents: Tetrahydrofuran; < 40 °C; 60 Min,25 °C2.2 0.1 H,25 °C; 4 H,25 °C2.3 Reagents: Hydrochloric Acid Solvents: Water; Rt 标题:Development Of Potential Manufacturing Routes For Substituted Thiophenes - Preparation Of Halogenated 2-Thiophenecarboxylic Acid Derivatives As Building Blocks For A New Family Of 2,6-Dihaloaryl 1,2,4-Triazole Insecticides 作者:Hull,John W. Jr.; Et Al 参考文献:Beilstein Journal Of Organic Chemistry 日期:2007 卷标:3]
23806-24-8 + 14282-78-1 = 81452-54-2 + 28686-90-0 反应条件:1.1 Catalysts: Sulfuric Acid Solvents: Methanol 标题:Synthesis Of N-(Methoxycarbonylthienylmethyl)Thioureas And Evaluation Of Their Interaction With Inducible And Neuronal Nitric Oxide Synthase 作者:Suaifan,Ghadeer A. R. Y.; Et Al 参考文献:Molecules 日期:2010 卷标:15 页码:3121-3134]
= 81452-54-2 + 28686-90-0 反应条件:1.1 Reagents: Butyllithium Solvents: Diethyl Ether,Hexane; 0 °C; 3 H,0 °C1.2 Solvents: Diethyl Ether; 0 °C; 16 H,0 °C1.3 Reagents: Water; Cooled 标题:Synthesis Of N-(Methoxycarbonylthienylmethyl)Thioureas And Evaluation Of Their Interaction With Inducible And Neuronal Nitric Oxide Synthase 作者:Suaifan,Ghadeer A. R. Y.; Et Al 参考文献:Molecules 日期:2010 卷标:15 页码:3121-3134
专利号:US-2024199637-A1 优先权日:2021-04-21 标题 :Improved process for the preparation of 7-(morpholinyl)-2-(n-piperazinyl)methylthieno[2, 3-c]pyridine derivatives 发明人:KOMPELLA AMALA; VAGICHERLA KAMESWARA RAO; LANKI REDDY TIRUMALA REDDY; PESARU NARMADA; MUDDASANI PULLA REDDY; NANNAPANENI VENKAIAH CHOWDARY 权利人:NATCO PHARMA LTD 摘要:The present invention describes an improved second generation process for the synthesis of NRC-1111 (1,5-[2-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-7-(4-morpholinyl)thieno[2,3-c] pyridine-5-yl]-2-pyrimidinamine) dimethane sulfonate and NRC-1109 (II, 5-[3-methyl-2-[(4-methylsulfonylpiperazin-1-yl)methyl]-7-morpholino-thieno[2,3-c]pyridin-5-yl]pyrimidin-2-amine) dimethane sulfonate. This process is cost effective, high yielding and industrially feasible process for the synthesis of compounds of formulae I and II with high purity. Formula (I) Formula (I): Râ•?H for NRC-1111 and Formula (II): Râ•?CH3 for NRC-1109 NRC-1111 and NRC-1109 are potential anti-cancer agents.
专利号:US-9695191-B2 优先权日:2009-08-05 标题 :Conformationally constrained, fully synthetic macrocyclic compounds 发明人:OBRECHT DANIEL; ERMERT PHILIPP; OUMOUCH SAID; LACH FRANCK; LUTHER ANATOL; MARX KARSTEN; MÖHLE KERSTIN 权利人:OBRECHT DANIEL; ERMERT PHILIPP; OUMOUCH SAID; LACH FRANCK; LUTHER ANATOL; MARX KARSTEN; MÖHLE KERSTIN; POLYPHOR AG 摘要:Conformationally restricted, spatially defined 12-30 membered macrocyclic ring systems of type (I) are constituted by three distinct building blocks: an aromatic template a, a conformation modulator b and a spacer moiety c as detailed in the description and the claims. Macrocycles of type (I) are readily manufactured by parallel synthesis or combinatorial chemistry. They are designed to interact with specific biological targets. In particular, they show agonistic or antagonistic activity on the motilin receptor (MR receptor), on the serotonin receptor of subtype 5-HT 2B (5-HT 2B receptor), and on the prostaglandin F2•receptor (FP receptor). They are thus potentially useful for the treatment of hypomotility disorders of the gastrointestinal tract such as diabetic gastroparesis and constipation type irritable bowl syndrome; of CNS related diseases like migraine, schizophrenia, psychosis or depression; of ocular hypertension such as associated with glaucoma and preterm labour.
专利号:WO-2010065383-A1 优先权日:2008-11-25 标 题 :Calcilytic compounds 发明人:CASILLAS LINDA N; CHARNLEY ADAM KENNETH; HARRIS PHILIP ANTHONY; JEONG JAE U; MARQUIS ROBERT W; RAMANJULU JOSHI M; TROUT ROBERT 权利人:GLAXOSMITHKLINE LLC; CASILLAS LINDA N; CHARNLEY ADAM KENNETH; HARRIS PHILIP ANTHONY; JEONG JAE U; MARQUIS ROBERT W; RAMANJULU JOSHI M; TROUT ROBERT 摘要:Novel calcilytic compounds, pharmaceutical compositions, methods of synthesis and methods of using them are provided.
专利号:CN-105111197-B 优先权日:2015-08-26 标 题:Synthesis method of raltitrexed