114650-12-3 = 948-65-2 反应条件:1.1 Reagents: Tetrabutylammonium Fluoride Solvents: Tetrahydrofuran; 3 H,Reflux 标题:Synthesis Of New Fused And Substituted Benzo And Pyrido Carbazoles Via C-2 (Het)Arylindoles 作者:Bourderioux,Aurelie; Kassis,Pamela; Merour,Jean-Yves; Routier,Sylvain 参考文献:Tetrahedron 日期:2008 卷标:64(49) 页码:11012-11019]
= 948-65-2 反应条件:1.1 Reagents: Ammonia Catalysts: Cuprous Iodide,Bis(Benzonitrile)Dichloropalladium,Tri-Tert-Butylphosphonium Tetrafluoroborate Solvents: Tetrahydrofuran,Water; 17 H,Rt1.2 Reagents: Hydrochloric Acid,Chloroauric Acid Solvents: Water; 24 H,Acidified,Rt1.3 Reagents: Sodium Carbonate Solvents: Water; Basified,Rt 标题:Effect Of The Use Of Bulky Alkylphosphines In The Sonogashira Coupling With Aqueous Ammonia 作者:Fukuoka,Sachio; Naito,Tetsuro; Sekiguchi,Hiroki; Somete,Takashi; Mori,Atsunori 参考文献:Heterocycles 日期:2008 卷标:76(1) 页码:819-826]
615-43-0 = 948-65-2 反应条件:1.1 Reagents: Triethylamine Catalysts: Palladium,Copper Solvents: Dimethylformamide,Water; 3 H,100 °C; 100 °C -> Rt 标题:New Hetero-Bimetallic Pd-Cu Catalysts For The One-Pot Indole Synthesis Via The Sonogashira Reaction 作者:Chouzier,Sandra; Gruber,Markus; Djakovitch,Laurent 参考文献:Journal Of Molecular Catalysis A: Chemical 日期:2004 卷标:212(1-2) 页码:43-52]
13141-38-3 = 948-65-2 反应条件:1.1 Reagents: Carbon Monoxide Catalysts: Cobalt,Compd. With Rhodium (2:2) Solvents: Toluene; 5 H,1 Atm,100 °C 标题:Heterobimetallic Cobalt/rhodium Nanoparticle-Catalyzed Carbonylative Cycloaddition Of 2-Alkynylanilines To Oxindoles 作者:Park,Ji Hoon; Kim,Eunha; Chung,Young Keun 参考文献:Organic Letters 日期:2008 卷标:10(21) 页码:4719-4721]
143360-89-8 = 948-65-2 反应条件:1.1 Reagents: Tripotassium Phosphate Catalysts: Tetrakis(Acetonitrile)Copper(1+) Hexafluorophosphate Solvents: Acetonitrile; 2.5 H,80 °C 标题:A Commercially Available And User-Friendly Catalyst For Hydroamination Reactions Under Technical Conditions 作者:Zelenay,Benjamin; Munton,Peter; Tian,Xiaojie; Diez-Gonzalez,Silvia 参考文献:European Journal Of Organic Chemistry 日期:2019 卷标:2019(29) 页码:4725-4730]
13141-38-3 = 948-65-2 反应条件:1.1 Catalysts: Potassium Tetrakis[3,5-Bis(Trifluoromethyl)Phenyl]Borate,1808207-42-2 Solvents: Benzene-D6; 1 H,Rt 标题:Diverse Reactivity Of A Tricoordinate Organoboron L2Phb: (L = Oxazol-2-Ylidene) Towards Alkali Metal,Group 9 Metal,And Coinage Metal Precursors 作者:Kong,Lingbing; Ganguly,Rakesh; Li,Yongxin; Kinjo,Rei 参考文献:Chemical Science 日期:2015 卷标:6(5) 页码:2893-2902]
937-33-7 + 70-11-1 = 948-65-2 反应条件:1.1 10 Min,20 Psi,150 °C 标题:Regiochemistry Of The Microwave-Assisted Reaction Between Aromatic Amines And α-Bromo Ketones To Yield Substituted 1H-Indoles 作者:Vara,Yosu; Aldaba,Eneko; Arrieta,Ana; Pizarro,Jose L.; Arriortua,Maria I.; Et Al 参考文献:Organic & Biomolecular Chemistry 日期:2008 卷标:6(10) 页码:1763-1772]
215997-72-1 = 948-65-2 反应条件:1.1 Reagents: Tetrabutylammonium Fluoride Solvents: Tetrahydrofuran1.2 Reagents: Water 标题:Convenient Synthesis Of 2-Substituted Indoles From 2-Ethynylanilines With Tetrabutylammonium Fluoride 作者:Yasuhara,Akito; Kanamori,Yuichi; Kaneko,Masashi; Numata,Atsushi; Kondo,Yoshinori; Et Al 参考文献:Journal Of The Chemical Society 日期:1999 卷标:(4) 页码:529-534]
120-72-9 + 98-80-6 = 948-65-2 反应条件:1.1 Catalysts: 2,9-Dimethyl-1,10-Phenanthroline,Palladium Diacetate Solvents: 1,2-Dichloroethane; 24 H,80 °C 标题:Ligand-Controlled Regiodivergent Direct Arylation Of Indoles Via Oxidative Boron Heck Reaction 作者:Yang,Yo-Sep; Lee,Sangmin; Son,Seung Hwan; Yoo,Hyung-Seok; Jang,Yoon Hu; Et Al 参考文献:Organic Chemistry Frontiers 日期:2022 卷标:9(21) 页码:5906-5911]
615-43-0 = 948-65-2 反应条件:1.1 Reagents: Pyridine Solvents: 1,2-Dichloroethane1.2 Reagents: Triethylamine,Cuprous Iodide Catalysts: Dichlorobis(Triphenylphosphine)Palladium Solvents: Dimethylformamide1.3 Reagents: Tetrabutylammonium Fluoride Solvents: Tetrahydrofuran1.4 Solvents: Ethyl Acetate 标题:Facile Solid-Phase Construction Of Indole Derivatives Based On A Traceless,Activating Sulfonyl Linker 作者:Zhang,Han-Cheng; Ye,Hong; Moretto,Alessandro F.; Brumfield,Kimberly K.; Maryanoff,Bruce E. 参考文献:Organic Letters 日期:2000 卷标:2(1) 页码:89-92]
615-43-0 = 948-65-2 + 886-66-8 反应条件:1.1 Reagents: Sodium Acetate,Cuprous Iodide Catalysts: Iron Oxide (Fe3O4),Palladium Solvents: Dimethylacetamide; 6 H,166 °C 标题:Efficient Synthesis Of Indole Derivatives Via Tandem Cyclization Catalyzed By Magnetically Recoverable Palladium/magnetite (Pd-Fe3O4) Nanocrystals 作者:Kwon,Jungmin; Chung,Jooyoung; Byun,Sangmoon; Kim,B. Moon 参考文献:Asian Journal Of Organic Chemistry 日期:2016 卷标:5(4) 页码:470-476]
98-80-6 + 139409-34-0 = 948-65-2 反应条件:1.1 Reagents: Tripotassium Phosphate Catalysts: Palladium Diacetate,2-Dicyclohexylphosphino-2′,6′-Dimethoxybiphenyl Solvents: Toluene; 1 H,90 °C 标题:A Highly Selective Tandem Cross-Coupling Of Gem-Dihaloolefins For A Modular,Efficient Synthesis Of Highly Functionalized Indoles 作者:Fang,Yuan-Qing; Lautens,Mark 参考文献:Journal Of Organic Chemistry 日期:2008 卷标:73(2) 页码:538-549]
15582-97-5 = 948-65-2 反应条件:1.1 Catalysts: Palladium Solvents: Diglyme; 20 H,180 °C 标题:Iridium Catalyzed Synthesis Of Tetrahydro-1H-Indoles By Dehydrogenative Condensation 作者:Forberg,Daniel; Kallmeier,Fabian; Kempe,Rhett 参考文献:Inorganics 日期:2019 卷标:7(8)]
143321-89-5 = 948-65-2 反应条件:1.1 Reagents: Cesium Carbonate Catalysts: Triphenylphosphine,2130844-30-1 Solvents: Toluene; 16 H,Reflux 标题:Immobilization Of Copper Complexes With (1,10-Phenanthrolinyl)Phosphonates On Titania Supports For Sustainable Catalysis 作者:Mitrofanov,Alexander; Brandes,Stephane; Herbst,Frederic; Rigolet,Severinne; Bessmertnykh-Lemeune,Alla; Et Al 参考文献:Journal Of Materials Chemistry A: Materials For Energy And Sustainability 日期:2017 卷标:5(24) 页码:12216-12235]
1310708-93-0 = 948-65-2 反应条件:1.1 Reagents: Sodium Ethoxide Solvents: Dimethyl Sulfoxide; 110 °C1.2 Solvents: Water 标题:Highly Efficient Synthesis Of A Novel Indolo [2,1-A] Isoquinoline Derivative Via C-H Activation Strategy 作者:Wang,Liang; Chen,Yu-Ting; Du,Yi-Na; Gu,Chang-Han; Peng,Wang-Ming 参考文献:Huaxue Yu Shengwu Gongcheng 日期:2015 卷标:32(9) 页码:19-22]
120-72-9 + 16919-18-9 + 10182-84-0 = 948-65-2 反应条件:1.1 Catalysts: 1786399-20-9 Solvents: Acetic Acid; 5 Min,298 K1.2 24 H,298 K 标题:Benzoato And Thiobenzoato Ligands In The Synthesis Of Dinuclear Palladium(Iii) And -(Ii) Compounds: Stability And Catalytic Applications 作者:Estevan,Francisco; Ibanez,Susana; Ofori,Albert; Hirva,Pipsa; Sanau,Mercedes; Et Al 参考文献:European Journal Of Inorganic Chemistry 日期:2015 卷标:2015(17) 页码:2822-2832]
1310708-93-0 = 948-65-2 反应条件:1.1 Reagents: Sodium Ethoxide Solvents: Dimethyl Sulfoxide; 2 H,110 °C; 110 °C -> Rt1.2 Reagents: Water; Rt 标题:Rhodium-Catalyzed Regioselective Direct C-H Arylation Of Indoles With Aryl Boronic Acids 作者:Wang,Liang; Qu,Xing; Li,Zhan; Peng,Wang-Ming 参考文献:Tetrahedron Letters 日期:2015 卷标:56(24) 页码:3754-3757]
120-72-9 + 16919-18-9 + 10182-84-0 = 948-65-2 反应条件:1.1 Catalysts: Stereoisomer Of Bis[μ-[1,3-Bis(2-Methylphenyl)-1-Triazenato-Kn1:Kn3]]Bis[μ-[2-(D... Solvents: Acetic Acid; 5 Min,298 K1.2 Solvents: Dichloromethane; 24 H,298 K 标题:Triazenides As Suitable Ligands In The Synthesis Of Palladium Compounds In Three Different Oxidation States: I,Ii,And Iii 作者:Ibanez,Susana; Oresmaa,Larisa; Estevan,Francisco; Hirva,Pipsa; Sanau,Mercedes; Et Al 参考文献:Organometallics 日期:2014 卷标:33(19) 页码:5378-5391
专利号:US-2008146656-A1 优先权日:2005-06-01 标题:Use of a steroid sulphatase inhibitor for inhibiting the synthesis of androstenedione and/or testosterone 发明人:REED MICHAEL JOHN; PUROHIT ATUL; WOO LOK WAI LAWRENCE; POTTER BARRY VICTOR LLOYD 权利人:REED MICHAEL JOHN; PUROHIT ATUL; WOO LOK WAI LAWRENCE; POTTER BARRY VICTOR LLOYD 摘要:There is provided use of a compound capable of inhibiting a steroid sulphatase enzyme (E.C.3.1.6.2) in the manufacture of a medicament for inhibiting in vivo synthesis of at least one of androstenedione and testosterone, which may be useful for the treatment of hirsutism, excess sebum production, benign breast disease, benign ovarian disease, polycystic ovarian disease and female infertility among others.
专利号:US-2024336649-A1 优先权日:2021-06-21 标 题 :Synthesis of covalent protein dimers that can inhibit myc-driven transcription 发明人:LOAS ANDREI; PENTELUTE BRADLEY L; POMPLUN SEBASTIAN; JBARA MUHAMMAD; SCHISSEL CARLY KATHERINE; RODRIQUEZ JACOB JOSHUA LEE; BUCHWALD STEPHEN LEFFLER; BOIJA ANN; KLEIN ISAAC; HAWKEN SUSANA WILSON; LI CHARLES HAN 权利人:MASSACHUSETTS INST TECHNOLOGY; WHITEHEAD INSTITUTE OF BIOMEDICAL RES 摘要:The disclosure relates to covalent protein dimers of MYC, MAX, and Omomyc; pharmaceutical compositions comprising the covalent protein dimers; methods of making the covalent protein dimers; and methods of treating disorders associated with MYC dysregulation (e.g., cancer) with the covalent protein dimers.
专利号:US-11851651-B2 优先权日:2017-06-19 标 题 :Automated methods for scalable, parallelized enzymatic biopolymer synthesis and modification using microfluidic devices 发明人:BANAL JAMES; BERLEANT JOSEPH DON; SHEPHERD TYSON; BATHE MARK 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:Methods for the automated template-free synthesis of user-defined sequence controlled biopolymers using microfluidic devices are described. The methods facilitate simultaneous synthesis of up to thousands of uniquely addressed biopolymers from the controlled movement and combination of regents as fluid droplets using microfluidic and EWOD-based systems. In some forms, biopolymers including nucleic acids, peptides, carbohydrates, and lipids are synthesized from step-wise assembly of building blocks based on a user-defined sequence of droplet movements. In some forms, the methods synthesize uniquely addressed nucleic acids of up to 1,000 nucleotides in length. Methods for adding, removing and changing barcodes on biopolymers are also provided. Biopolymers synthesized according to the methods, and libraries and databases thereof are also described. Modified biopolymers, including chemically modified nucleotides and biopolymers conjugated to other molecules are described.
专利号:US-10556913-B2 优先权日:2015-07-21 标 题:Asymmetric process for the preparation of thieno-indoles derivatives 发明人:BERIA ITALO; CARUSO MICHELE; DONATI DANIELE; ORSINI PAOLO 权利人:NERVIANO MEDICAL SCIENCES SRL 摘要:The present invention relates to a new process for the preparation of thieno-indole derivatives of formula (Ia) or (Ib), exploiting an asymmetric synthesis for the preparation of key (8S) or (8R) 8-(halomethyl)-1-alkyl-7,8-dihydro-6H-thieno[3,2-e]indol-4-ol intermediates, and to useful intermediate compounds of such process. n Thieno-indole derivatives are described and claimed in GB2344818, WO2013/149948 and WO2013/149946, which also disclose processes for their preparation. n Thieno-indole enantiopure derivatives can now be advantageously prepared through a new asymmetric synthesis of the key 8-(halomethyl)-7,8-dihydro-6H-thieno[3,2-e]indol intermediates, which, avoiding the chiral resolution step, provides benefits in terms of reducing time and costs of the whole process for their preparation. The synthesis starts from the N-alkylation of 5-amino-4-halo-3-alkyl-1-benzothiophene-7-ol derivatives with enantiopure glycidyl 3-nosylate, followed by intramolecular 6-endo-tet cyclization using alkyl Grignard reagents; Mitsunobu activation of the secondary alcohol promotes internal spirocyclization, affording the 4,4a,5,6-tetrahydro-8H-cyclopropa[c]thieno[3,2-e]indol-8-one derivatives; finally, stereo-electronically controlled regioselective cyclopropane opening yields the key enantiopure 8-(halomethyl)-1-alkyl-7,8-dihydro-6H-thieno[3,2-e]indol-4-ol intermediates; which can be further derivatized following teachings disclosed in WO2013/149948 or WO2013/149946, to prepare the final thieno-indole derivatives of formula (Ia) or (Ib). n Such compounds are disclosed to be alkylating compounds with cytotoxic activity, therefore useful as such in the treatment of a variety of cancers and in cell proliferative disorders, or, conjugated with different types of nucleophiles, in the preparation of Antibody Drug Conjugated derivatives.
专利号:US-5144073-A 优先权日:1988-08-31 标 题 :Process for preparation of dipeptides 发明人:HUBBS JOHN C 权利人:HUBBS JOHN C 摘要:Disclosed is a process for synthesis of a dipeptide such as N-acetyl-L- alpha -aspartyl-L-phenylalanine methyl ester wherein one amino acid serves as a chiral template which allows for synthesis of a second amino acid residue to form said dipeptide. The process involves several novel steps such as a nucleophile addition step. In addition, several novel intermediates are described.
专利号:US-2022233673-A1 优先权日:2019-06-04 标 题:METHODS OF PRODUCING SHIGA TOXIN B-SUBUNIT (STxB) MONOMERS AND OLIGOMERS, AND USES THEREOF 发明人:BILLET ANNE; SCHMIDT FRÉDÉRIC; JOHANNES LUDGER; SERVENT DENIS; MOURIER GILLES; TARTOUR ÉRIC; KAY MICHAEL; FULCHER JAMES M 权利人:INST CURIE; CENTRE NAT RECH SCIENT; INST NAT SANTE RECH MED; COMMISSARIAT A LENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES CEA; APHP ASSIST PUBLIQUE HOPITAUX DE PARIS; UNIV PARIS; UNIV OF UTAH RESEARCH FOUDATION; UNIV UTAH RES FOUND 摘要:A method of producing a monomer of a Shiga toxin B-subunit (STxB) protein or of a variant thereof by peptide chemical synthesis, as well as to a method of producing a pentamer of the STxB protein or of the variant thereof. The methods are particularly advantageous as they overcome major issues typically observed in peptide chemical synthesis, including solubility and purity issues.
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合成参考文献
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