685-87-0 = 87-13-8 [标题:Reaction Conditions 标题:Reaction Of Orthoformates With Acidic Methines 作者:Swaringen,Roy A. Jr.; Et Al 参考文献:Journal Of Organic Chemistry 日期:1979 卷标:44(26) 页码:4825-9]
105-53-3 = 87-13-8 反应条件:1.1 Reagents: Acetic Anhydride Catalysts: Zinc (Activated Clay-Supported) 标题:Study On Condensation Reactivity Of Supported Zinc Catalysts 作者:Xiao,Cuo-Min; Et Al 参考文献:Huaxue Yanjiu 日期:2001 卷标:12(4) 页码:26-28]
28783-51-9 = 87-13-8 [标题:Reaction Conditions 标题:Product Subclass 3: Enol Ethers 作者:Milata,V.; Et Al 参考文献:Science Of Synthesis 日期:2008 卷标:32 页码:589-756]
141-82-2 = 87-13-8 反应条件:1.1 Reagents: Sulfamic Acid,Sulfuric Acid Solvents: Cyclohexane; 3 H,Reflux2.1 Reagents: Acetic Anhydride,Zinc Chloride; 4 H,Reflux 标题:Design,Synthesis,And Dual Evaluation Of Quinoline And Quinolinium Iodide Salt Derivatives As Potential Anticancer And Antibacterial Agents 作者:Jin,Guofan; Et Al 参考文献:Chemmedchem 日期:2020 卷标:15(7) 页码:600-609
7-(4-吗啉基甲基)-3,4-二氢-2H-1,4-苯并恶嗪 反应生成 乙氧基甲叉丙二酸二乙酯 参考文献:Thioxazinoquinolones As Antiviral Agents 标题:Thioxazinoquinolones As Antiviral Agents 摘要:本发明提供了一种化合物,其化学式为i1.这些化合物可用作抗病毒药物,特别是用于对抗疱疹病毒家族的药物.
专利号:WO-9517903-A1 优先权日:1993-12-28 标 题:Modular design and synthesis of oxazolone-derived molecules 发明人:HOGAN JOSEPH C JR; CASEBIER DAVID; FURTH PAUL; TU CHENG 权利人:ARQULE PARTNERS L P; HOGAN JOSEPH C JR; CASEBIER DAVID; FURTH PAUL; TU CHENG 摘要:The design and synthesis of novel oxazolone-derived molecular modules and the use of the modules in the construction of new molecules and fabricated materials is disclosed. The new molecules and fabricated materials are molecular recognition agents useful in the design and synthesis of drugs, and have applications in separations and materials science.
专利号:US-5521310-A 优先权日:1992-10-07 标 题 :Process to obtain benzoxazines to be used for the synthesis of ofloxazine, levofloxazine and derivatives 发明人:CARRETERO GONZALVEZ JUAN-CARLO; VICIOSO SANCHEZ MERCEDES; GARCIA RUANO JOSE-LUIS 权利人:ETILO DERIVADOS 摘要:A process to obtain benzoxazines useful for the synthesis of Ofloxazine, Levofloxazine and derivatives. The benzoxacines (I) where Xb is an halogen and R 1 is H, alkyl or alkenyl of up to 6 atoms of C or aryl, can be obtained by means of cycling a compound of formula (II) through the reaction with triphenylphosphine and ethyl azodicarboxilate. The compounds of formula (II) can be obtained through the reaction of a compound (III) with an adequate epoxide. Through the use of the adequate chiral epoxide it is possible to obtain the enantiomerically desired intermediate and, therefore and selectively, it is possible to obtain the desired final product with the adequate enantiomeric form without the need to carry out a resolution stage. n The Compounds (I) are useful and key intermediates for the synthesis of the antimicrobials Oflixazine and Levofloxazine. ##STR1##
专利号:US-10336703-B2 优先权日:2015-05-12 标题 :Process for the synthesis of ivacaftor and related compounds 发明人:REDDY DUMBALA SRINIVASA; NATARAJAN VASUDEVAN; JACHAK GORAKHNATH RAJARAM 权利人:COUNCIL SCIENT IND RES 摘要:The present patent discloses a novel one pot two-step process for the synthesis of ivacaftor and related compounds of [Formula (I)], wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and Ar 1 are as described above; its tautomers or pharmaceutically acceptable salts thereof starting from indole acetic acid amides.
专利号:US-4699984-A 优先权日:1984-09-17 标 题 :Preparation of intermediates to 6-fluoro-7-(2,6-dimethylpyridyl)quinoline carboxylic acids and compounds 发明人:SINGH BALDEV 权利人:STERLING DRUG INC 摘要:Shown is the process which comprises heating 4-(2-fluorophenyl)-2,6-dimethyl-3,5-pyridinedicarboxylic acid to produce a mixture of 4-(2-fluorophenyl)-2,6-dimethylpyridine and 2,4-dimethyl-5H-[1]benzopyrano[3,4-c]pyridin-5-one, separating the components of said mixture and nitrating 4-(2-fluorophenyl)-2,6-dimethylpyridine to produce 4-(2-fluoro-5-nitrophenyl)-2,6-dimethylpyridine. Also shown are the 3-step synthesis of 4-(2-fluorophenyl)-2,6-dimethyl-3,5-pyridinedicarboxylic acid from 2-fluorobenzaldehyde and the five step synthesis of 1-ethyl-6-fluoro-1,4-dihydro-7-(2,6-dimethyl-4-pyridinyl)-4-oxo-3-quinolinecarboxylic acid, a highly potent antibacterial agent, starting with 4-(2-fluoro-5-nitrophenyl)-2,6-dimethylpyridine. Other intermediates shown in said five step synthesis include 3-(2,6-dimethyl-4-pyridinyl)-4-fluorobenzeneamine and diethyl 4-fluoro-3-(2,6-dimethyl-4-pyridinyl)anilinomethylenemalonate.
专利号:US-6465653-B2 优先权日:1998-09-29 标题:Noncatalyzed synthesis of 4-hydroxyquinolines and/or tautomers thereof 发明人:DANG TAUN-PHAT; ROUSTAN ALAIN 权利人:RHODIA CHIMIE SA 摘要:The 4-hydroxyquinoline compounds and/or tautomers thereof, notably 4-hydroxy-5,7-dichchloroquinoline, are synthesized in very high yields by hydrolyzing/decarboxylating a 4-hydroxyquinolinecarboxylic acid ester in the presence of water, whether in liquid or vapor state, but in the absence of any catalyst for such reaction(s).
专利号:US-7897762-B2 优先权日:2006-09-14 标 题:Kinase inhibitors useful for the treatment of proliferative diseases 发明人:FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C 权利人:DECIPHERA PHARMACEUTICALS LLC 摘要:The present invention relates to novel kinase inhibitors and modulator compounds useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.
[参考文献]: Cristina Megías, Et Al. Determination Of L-Canavanine And Other Free Amino Acids In Vicia Disperma (Fabaceae) Seeds By Precolumn Derivatization Using Diethyl Ethoxymethylenemalonate And Reversed-Phase High-Performance Liquid Chromatography. Talanta. 2015 Jan:131:95-8. [参考文献]: Hyun Joong Kim, Et Al. Optimization Of Direct Lysine Decarboxylase Biotransformation For Cadaverine Production With Whole-Cell Biocatalysts At High Lysine Concentration. J Microbiol Biotechnol. 2015 Jul;25(7):1108-13. [参考文献]: J L Ordóez, Et Al. Impact Of Gluconic Fermentation Of Strawberry Using Acetic Acid Bacteria On Amino Acids And Biogenic Amines Profile. Food Chem. 2015 Jul 1:178:221-8. [参考文献]: Ke Tang, Et Al. Brief Report: Human Mesenchymal Stem-Like Cells Facilitate Floating Tumorigenic Cell Growth Via Glutamine-Ammonium Cycle. Stem Cells. 2015 Sep;33(9):2877-84. [参考文献]: Maarja-Liisa Oldekop, Et Al. Study Of The Matrix Effects And Sample Dilution Influence On The Lc-Esi-Ms/ms Analysis Using Four Derivatization Reagents. J Chromatogr B Analyt Technol Biomed Life Sci. 2014 Sep 15:967:147-55.
合成参考文献
摘要:Harris, P. A., Science of Synthesis Knowledge Updates, (2021) 3, 187. 摘要:Harris, P. A., Science of Synthesis Knowledge Updates, (2021) 3, 91. 摘要:von Angerer, S., Science of Synthesis Knowledge Updates, (2011) 1, 171. 摘要:Arndtsen, B. A.; Tjutrins, J., Science of Synthesis: Multicomponent Reactions, (2013) 2, 477. 摘要:National Defense Research Committee, Office of Scientific Research and Development, Progress Report., 30101(11), 1945