4740-00-5 = 872-93-5 反应条件:1.1 Reagents: Hydrogen Peroxide 标题:Method For The Preparation Of 2- And 3-Alkyl(Cycloalkyl Or Phenyl)Thiophanes 作者:Volynskii,N. P.; Et Al 参考文献:Izvestiya Akademii Nauk Sssr 日期:1979 卷标:(5) 页码:1080-5]
720719-27-7 = 872-93-5 反应条件:1.1 Solvents: Benzene; Reflux1.2 Reagents: Tributylstannane Catalysts: Azobisisobutyronitrile Solvents: Benzene; 30 Min,Reflux; 60 Min,Reflux1.3 Reagents: Carbon Tetrachloride 标题:The Regiochemistry Of Cyclization Of α-Sulfenyl-,α-Sulfinyl-,And α-Sulfonyl-5-Hexenyl Radicals: Procedures Leading To Regioselective Syntheses Of Cyclic Sulfones And Sulfoxides 作者:Della,Ernest W.; Et Al 参考文献:Journal Of Organic Chemistry 日期:2004 卷标:69(11) 页码:3824-3835]
23974-72-3 + 720719-20-0 = 872-93-5 反应条件:1.1 Reagents: Sodium Periodate Solvents: Acetone,Water; 0 °C; 2 H,0 °C -> Rt1.2 Reagents: Triethylamine,Methanesulfonyl Chloride; 3 H,Rt1.3 Solvents: Diethyl Ether; Rt1.4 Solvents: Ethanol; Overnight,Rt2.1 Solvents: Benzene; Reflux2.2 Reagents: Tributylstannane Catalysts: Azobisisobutyronitrile Solvents: Benzene; 30 Min,Reflux; 60 Min,Reflux2.3 Reagents: Carbon Tetrachloride 标题:The Regiochemistry Of Cyclization Of α-Sulfenyl-,α-Sulfinyl-,And α-Sulfonyl-5-Hexenyl Radicals: Procedures Leading To Regioselective Syntheses Of Cyclic Sulfones And Sulfoxides 作者:Della,Ernest W.; Et Al 参考文献:Journal Of Organic Chemistry 日期:2004 卷标:69(11) 页码:3824-3835]
148420-02-4 = 872-93-5 反应条件:1.1 Reagents: Disodium Sulfide Solvents: Ethanol,Water2.1 Reagents: (Dimethyl Sulfide)Trihydroboron; 0 °C; 1 H,Rt; Rt -> 0 °C2.2 Reagents: Sodium Hydroxide,Hydrogen Peroxide Solvents: Water; 0 °C -> Rt; 2 H,Rt3.1 Reagents: Sodium Periodate Solvents: Acetone,Water; 0 °C; 2 H,0 °C -> Rt3.2 Reagents: Triethylamine,Methanesulfonyl Chloride; 3 H,Rt3.3 Solvents: Diethyl Ether; Rt3.4 Solvents: Ethanol; Overnight,Rt4.1 Solvents: Benzene; Reflux4.2 Reagents: Tributylstannane Catalysts: Azobisisobutyronitrile Solvents: Benzene; 30 Min,Reflux; 60 Min,Reflux4.3 Reagents: Carbon Tetrachloride 标题:The Regiochemistry Of Cyclization Of α-Sulfenyl-,α-Sulfinyl-,And α-Sulfonyl-5-Hexenyl Radicals: Procedures Leading To Regioselective Syntheses Of Cyclic Sulfones And Sulfoxides 作者:Della,Ernest W.; Et Al 参考文献:Journal Of Organic Chemistry 日期:2004 卷标:69(11) 页码:3824-3835]
321979-37-7 = 872-93-5 反应条件:1.1 Reagents: Tributylstannane Catalysts: Azobisisobutyronitrile Solvents: Benzene; 5 Min,Reflux; 60 Min,Reflux1.2 Reagents: Carbon Tetrachloride 标题:The Regiochemistry Of Cyclization Of α-Sulfenyl-,α-Sulfinyl-,And α-Sulfonyl-5-Hexenyl Radicals: Procedures Leading To Regioselective Syntheses Of Cyclic Sulfones And Sulfoxides 作者:Della,Ernest W.; Et Al 参考文献:Journal Of Organic Chemistry 日期:2004 卷标:69(11) 页码:3824-3835]
= 872-93-5 反应条件:1.1 Reagents: Carbon Tetrabromide,Triphenylphosphine Solvents: Dichloromethane; 0 °C; Overnight,0 °C1.2 Reagents: Methyl Iodide Solvents: Diethyl Ether2.1 Reagents: Tributylstannane Catalysts: Azobisisobutyronitrile Solvents: Benzene; 5 Min,Reflux; 60 Min,Reflux2.2 Reagents: Carbon Tetrachloride 标题:The Regiochemistry Of Cyclization Of α-Sulfenyl-,α-Sulfinyl-,And α-Sulfonyl-5-Hexenyl Radicals: Procedures Leading To Regioselective Syntheses Of Cyclic Sulfones And Sulfoxides 作者:Della,Ernest W.; Et Al 参考文献:Journal Of Organic Chemistry 日期:2004 卷标:69(11) 页码:3824-3835]
54462-66-7 = 872-93-5 反应条件:1.1 Reagents: Disodium Sulfide2.1 Reagents: Hydrogen Peroxide 标题:Method For The Preparation Of 2- And 3-Alkyl(Cycloalkyl Or Phenyl)Thiophanes 作者:Volynskii,N. P.; Et Al 参考文献:Izvestiya Akademii Nauk Sssr 日期:1979 卷标:(5) 页码:1080-5]
143435-56-7 = 872-93-5 反应条件:1.1 Reagents: (Dimethyl Sulfide)Trihydroboron; 0 °C; 1 H,Rt; Rt -> 0 °C1.2 Reagents: Sodium Hydroxide,Hydrogen Peroxide Solvents: Water; 0 °C -> Rt; 2 H,Rt2.1 Reagents: Sodium Periodate Solvents: Acetone,Water; 0 °C; 2 H,0 °C -> Rt2.2 Reagents: Triethylamine,Methanesulfonyl Chloride; 3 H,Rt2.3 Solvents: Diethyl Ether; Rt2.4 Solvents: Ethanol; Overnight,Rt3.1 Solvents: Benzene; Reflux3.2 Reagents: Tributylstannane Catalysts: Azobisisobutyronitrile Solvents: Benzene; 30 Min,Reflux; 60 Min,Reflux3.3 Reagents: Carbon Tetrachloride 标题:The Regiochemistry Of Cyclization Of α-Sulfenyl-,α-Sulfinyl-,And α-Sulfonyl-5-Hexenyl Radicals: Procedures Leading To Regioselective Syntheses Of Cyclic Sulfones And Sulfoxides 作者:Della,Ernest W.; Et Al 参考文献:Journal Of Organic Chemistry 日期:2004 卷标:69(11) 页码:3824-3835]
71052-94-3 = 872-93-5 反应条件:1.1 Reagents: Phosphorus Tribromide,Hydrogen Bromide2.1 Reagents: Disodium Sulfide3.1 Reagents: Hydrogen Peroxide 标题:Method For The Preparation Of 2- And 3-Alkyl(Cycloalkyl Or Phenyl)Thiophanes 作者:Volynskii,N. P.; Et Al 参考文献:Izvestiya Akademii Nauk Sssr 日期:1979 卷标:(5) 页码:1080-5]
720719-20-0 = 872-93-5 反应条件:1.1 Reagents: Sodium Periodate Solvents: Methanol,Water; 0 °C; 2 H,0 °C -> Rt2.1 Reagents: Carbon Tetrabromide,Triphenylphosphine Solvents: Dichloromethane; 0 °C; Overnight,0 °C2.2 Reagents: Methyl Iodide Solvents: Diethyl Ether3.1 Reagents: Tributylstannane Catalysts: Azobisisobutyronitrile Solvents: Benzene; 5 Min,Reflux; 60 Min,Reflux3.2 Reagents: Carbon Tetrachloride 标题:The Regiochemistry Of Cyclization Of α-Sulfenyl-,α-Sulfinyl-,And α-Sulfonyl-5-Hexenyl Radicals: Procedures Leading To Regioselective Syntheses Of Cyclic Sulfones And Sulfoxides 作者:Della,Ernest W.; Et Al 参考文献:Journal Of Organic Chemistry 日期:2004 卷标:69(11) 页码:3824-3835]
3565-66-0 = 872-93-5 反应条件:1.1 -2.1 Reagents: Phosphorus Tribromide,Hydrogen Bromide3.1 Reagents: Disodium Sulfide4.1 Reagents: Hydrogen Peroxide 标题:Method For The Preparation Of 2- And 3-Alkyl(Cycloalkyl Or Phenyl)Thiophanes 作者:Volynskii,N. P.; Et Al 参考文献:Izvestiya Akademii Nauk Sssr 日期:1979 卷标:(5) 页码:1080-5]
= 872-93-5 反应条件:1.1 -2.1 -3.1 Reagents: Phosphorus Tribromide,Hydrogen Bromide4.1 Reagents: Disodium Sulfide5.1 Reagents: Hydrogen Peroxide 标题:Method For The Preparation Of 2- And 3-Alkyl(Cycloalkyl Or Phenyl)Thiophanes 作者:Volynskii,N. P.; Et Al 参考文献:Izvestiya Akademii Nauk Sssr 日期:1979 卷标:(5) 页码:1080-5]
314056-83-2 = 872-93-5 + 4988-33-4 + 273754-86-2 反应条件:1.1 Reagents: Tributyltin Oxide1.2 Reagents: Tributylstannane 标题:Ring Closure Of 2-Thia- And 2-Sulfonyl-5-Hexenyl Radicals 作者:Della,Ernest W.; Et Al 参考文献:Tetrahedron Letters 日期:2000 卷标:41(41) 页码:7987-7990
专利号:US-2023391818-A1 优先权日:2020-11-05 标 题:Peptide synthesis method for suppressing defect caused by diketopiperazine formation 发明人:NOMURA KENICHI; KAGE MIRAI; TAMIYA MINORU; KANAZAWA JUNICHIRO 权利人:CHUGAI PHARMACEUTICAL CO LTD 摘要:Solid-phase synthesis of a peptide has a problem that a desired elongation reaction is prevented from proceeding by diketopiperazine and a 6-membered diamine skeleton compound formed when a protective group at the N-terminal is removed. The present inventors have found that when in production of a peptide by a solid-phase method, a peptide in which an amino group at the N-terminal is protected with a protective group having an Fmoc skeleton is treated in a specific solvent with a base having a pKa of 23 or more in acetonitrile as a conjugate acid, and a peptide chain is then elongated, it is possible to solve the problem described above.
专利号:WO-2020208409-A1 优先权日:2019-04-10 标 题 :Improved processes for the preparation of peptide intermediates/modifiers 发明人:BUDHDEV DR RAJEEV REHANI; NARIYAM MUNASWAMY SEKHAR; AKULA SWAPNA; KAIPU RAMAKRISHNA REDDY; KOMATI SHRAVAN KUMAR; KARTHIK RAMASWAMY; KOMARAVOLU YAGNA KIRAN KUMAR 权利人:Dr Reddy’s Laboratories Ltd 摘要:The present application relates to improved processes for the preparation of peptide intermediates/modifier compounds of Formula (I) and their use in the synthesis of peptide derivatives. The present application further provides the compound of Formula I with high chemical purity of >98% and chiral purity of >99% and its use to make pharmaceutical peptide like Liraglutide.
专利号:US-8653282-B2 优先权日:2007-10-18 标 题:Preparation of dihydrothieno [3,2-D] pyrimidines and intermediates used therein 发明人:FRUTOS ROGELIO; KRISHNAMURTHY DHILEEPKUMAR; MULDER JASON ALAN; RODRIGUEZ SONIA; SENANAYAKE CHRIS HUGH; TAMPONE THOMAS G 权利人:FRUTOS ROGELIO; KRISHNAMURTHY DHILEEPKUMAR; MULDER JASON ALAN; RODRIGUEZ SONIA; SENANAYAKE CHRIS HUGH; TAMPONE THOMAS G; BOEHRINGER INGELHEIM INT 摘要:The invention relates to improved methods of preparing dihydrothienopyrimidines of formula 1, and intermediates thereof, (I) wherein X is SO or SO 2 , preferably SO, and wherein R A , R 1 , R 2 , R 3 , R 4 and R 5 have the meanings given in the description. The methods according to this invention are more suitable for large-scale synthesis of said compounds than prior methods because the new synthetic process avoids distillation and chromatographic purification between steps and results in a higher overall yield of the desired product.
专利号:US-10927095-B2 优先权日:2017-08-14 标 题:Processes for the preparation of Niraparib and intermediates thereof 发明人:LUTHRA PARVEN K; VASOYA SANJAY L; PATIL BHATU T; TANEJA AMIT K; SRIVASTAV NAVEEN C; SINGH RINKU 权利人:TEVA PHARMACEUTICALS INT GMBH 摘要:The present invention relates to novel procedures and novel intermediates useful in the synthesis of Niraparib or any salt thereof.
专利号:US-4311862-A 优先权日:1979-09-04 标 题:Preparation of unsaturated ethers 发明人:DRENT EIT 权利人:SHELL OIL CO 摘要:Process for the preparation of olefinically unsaturated ethers by reacting a conjugated diene and a lower alkanol with the aid of an acidic catalyst in the presence of a non-basic aprotic polar solvent. The olefinically unsaturated ethers are of interest as solvents and gasoline additives and can also be used as starting materials for e.g. the synthesis of ketones.
专利号:WO-2023214577-A1 优先权日:2022-05-02 标 题 :Peptide synthesis method for suppressing defect caused by diketopiperazine formation 发明人:KAGE MIRAI; TAMIYA MINORU; KANAZAWA JUNICHIRO; NOMURA KENICHI 权利人:CHUGAI PHARMACEUTICAL CO LTD 摘要:The present invention addresses the problem of a desired elongation reaction not progressing as a result of a 6-membered cyclic amidine skeleton structure and a diketopiperazine formed when removing an N-terminated protective group during peptide synthesis. The inventors have discovered that it is possible to solve said problem during peptide production by treating a peptide protected by an N-terminated amino group in a protective group having an Fmoc skeleton by using a base which has a pKa of 23 or higher in an acetonitrile of a conjugate acid in a specific solvent, and next, performing peptide chain elongation.
参考文献:10.1186/s42834-023-00166-x 摘要:Wang C, Liang C, Liu Y, Yang C. Sulfolane degrading bacteria from petrochemical plant: activated sludge enrichment, isolation and characterization. Sustain Environ Res. 2023 Feb 15;33(1). doi: 10.1186/s42834-023-00166-x.