合成目标产物 Phthalide 主要起始原料 Carbon Monoxide And 2-Iodobenzyl Alcohol
87-24-1 = 87-41-2 + 96259-59-5 + 7115-91-5 反应条件:1.1 Reagents: N-Bromosuccinimide Solvents: Carbon Tetrachloride 标题:Substituent Effects On Hydrogenation Of Aromatic Rings: Hydrogenation Vs. Hydrogenolysis In Cyclic Analogs Of Benzyl Ethers 作者:Anzalone,Luigi; Hirsch,Jerry A. 参考文献:Journal Of Organic Chemistry 日期:1985 卷标:50(12) 页码:2128-33]
643-79-8 = 87-41-2 反应条件:1.1 Catalysts: 2144743-11-1 Solvents: Benzene-D6; 3 H,Rt1.2 Reagents: Methanol; Rt 标题:Synthesis,Characterization And Catalytic Performances Of Benzimidazolin-2-Iminato Actinide (Iv) Complexes In The Tishchenko Reactions For Symmetrical And Unsymmetrical Esters 作者:Liu,Heng; Khononov,Maxim; Fridman,Natalia; Tamm,Matthias; Eisen,Moris S. 参考文献:Journal Of Organometallic Chemistry 日期:2018 卷标:857 页码:123-137]
643-79-8 = 87-41-2 反应条件:1.1 Catalysts: (T-4)-[1,3-Bis[2,6-Bis(1-Methylethyl)Phenyl]-1,3-Dihydro-2H-Imidazol-2-Iminato-K... Solvents: Benzene-D6; 6 H,Rt1.2 Reagents: Oxygen Solvents: Methanol; Rt 标题:Mono(Imidazolin-2-Iminato) Actinide Complexes: Synthesis And Application In The Catalytic Dimerization Of Aldehydes 作者:Karmel,Isabell S. R.; Fridman,Natalia; Tamm,Matthias; Eisen,Moris S. 参考文献:Journal Of The American Chemical Society 日期:2014 卷标:136(49) 页码:17180-17192]
专利号:US-7329515-B2 优先权日:2003-04-21 标题 :Solid support for the synthesis of 3′-amino oligonucleotides 发明人:LEUCK MICHAEL; WOLTER ANDREAS 权利人:SIGMA ALDRICH CO 摘要:The present invention discloses novel methods and solid supports for the synthesis of 3′-amino oligonucleotides. The novel supports are based on an unsubstituted or ring-substituted hydroxymethylbenzoyl linker element wherein the hydroxymethyl group is esterified to a solid phase bound carboxylic acid and the carbonyl group is linked to an amino alcohol as an amide. Oligonucleotides are conveniently synthesized on the novel supports with no modifications in the standard phosphoramidite synthesis scheme. The ester function of the support is cleaved under the alkaline deprotection conditions for oligonucleotides to provide a free hydroxymethyl group that aids in the release of the 3′-amino oligonucleotide products with a free amino group through neighbor group participation. The free amino group of the oligonucleotides is available for further conjugation reactions to haptens, reporter groups, surfaces or other small molecules or biomolecules. The methods provided are particularly mild, do not require any modifications in standard protocols for the synthesis and deprotection of oligonucleotides, provide the 3′-amino oligonucleotides free of side products and do not introduce chiral centers to the oligonucleotides.
专利号:US-4288608-A 优先权日:1978-06-01 标题:Synthesis of anthracyclines 发明人:JOHNSON FRANCIS; KIM KYOUNG S 权利人:RESEARCH CORP 摘要:There is provided a novel method of synthesizing certain heterocyclic quinones. In particular there is provided a novel and regiospecific synthesis of 9-acetyl-6,11-dihydroxy-4-methoxy-7,8,9,10-tetrahydronaphthacene-5,12-quinone (7,9-dideoxydaunomycinone) which is known intermediate in the synthesis of daunomycinone. There is also provided a method of preparing analogs of 7,9-dideoxydaunomycinone which thus provide for the preparation of known and desired analogs of daunomycinone. Daunomycinone is a known compound which is an intermediate in the preparation of the clinically accepted naturally-occurring antitumor antibiotics daunomycin and its derivitive adriamycin.
专利号:US-11465970-B2 优先权日:2017-12-14 标题 :Method for synthesis of Roxadustat and intermediate compounds thereof 发明人:XU YONGXIANG 权利人:NANJING CAVENDISH BIO ENGINEERING TECH CO LTD; XU YONGXIANG; NANJING CAVENDISH BIO ENG TECH CO LTD 摘要:The present application provides a method for synthesis of Roxadustat. A compound as represented by formula (VIII) is used as a raw material, and is reacted with phenol, a vinyl-containing ether, an acid, hydroxylamine, and then the product is reacted with glycine. In addition, the present application also provides intermediate compounds as represented by formula (IX), formula (XI), formula (XII), formula (IV), and formula (V) for synthesis of Roxadustat. Herein, details of the substituents involved in formula (VIII), formula (IX), formula (XI), and formula (XII) are stated in the description
专利号:US-9688644-B2 优先权日:2009-04-30 标 题 :Synthesis of Tetracyclines and intermediates thereto 发明人:MYERS ANDREW G; KUMMER DAVID A; LI DERUN; HECKER EVAN; DION AMELIE; WRIGHT PETER M 权利人:HARVARD COLLEGE 摘要:The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides more efficient routes for preparing the enone intermediate and allows for substituents at positions 4a, 5, 5a, and 12a of the tetracycline ring system.
专利号:US-9884830-B2 优先权日:2004-05-21 标题 :Synthesis of tetracyclines and analogues thereof 发明人:MYERS ANDREW G; CHAREST MARK G; LERNER CHRISTIAN D; BRUBAKER JASON D; SIEGEL DIONICIO R 权利人:HARVARD COLLEGE 摘要:The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetracycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-proliferative agents in the treatment of diseases of humans or other animals.
专利号:US-8907104-B2 优先权日:2006-10-11 标 题 :Synthesis of enone intermediate 发明人:MYERS ANDREW G; BRUBAKER JASON D 权利人:HARVARD COLLEGE 摘要:The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides a more efficient route for preparing the enone intermediate.
[参考文献]: Chakapong Intaraudom, Et Al. Antimicrobial Drimane - Phthalide Derivatives From Hypoxylon Fendleri Bcc32408. Fitoterapia. 2019 Oct;138:104353. [参考文献]: Liu Zeng Chen, Et Al. Novel Phthalide Derivatives: Synthesis And Anti-Inflammatory Activity In Vitro And In Vivo. Eur J Med Chem. 2020 Nov 15;206:112722. [参考文献]: Xin Fang, Et Al. Synthesis Of Phthalide Derivatives And Evaluation On Their Antiplatelet Aggregation And Antioxidant Activities. J Asian Nat Prod Res. 2020 Dec;22(12):1176-1187. [参考文献]: Alejandra León, Et Al. Phthalides And Other Constituents From Ligusticum Porteri; Sedative And Spasmolytic Activities Of Some Natural Products And Derivatives. Nat Prod Res. 2011 Aug;25(13):1234-42. [参考文献]: Bin Xiao, Et Al. Design And Synthesis Of Marine Fungal Phthalide Derivatives As Ppar-γ Agonists. Bioorg Med Chem. 2012 Aug 15;20(16):4954-61.
合成参考文献
参考文献:10.3389/fmicb.2011.00096 摘要:Thywißen A, Heinekamp T, Dahse HM, Schmaler-Ripcke J, Nietzsche S, Zipfel PF, Brakhage AA. Conidial Dihydroxynaphthalene Melanin of the Human Pathogenic Fungus Aspergillus fumigatus Interferes with the Host Endocytosis Pathway. Front Microbiol. 2011;2():96. 参考文献:10.1021/ol201563r 摘要:Ackermann L, Pospech J. Ruthenium-catalyzed oxidative C-H bond alkenylations in water: expedient synthesis of annulated lactones. Org Lett. 2011 Aug 19;13(16):4153–5. doi: 10.1021/ol201563r.