1-(羟甲基)-4-甲氧基萘置于pyridinium Chlorochromate体系中,用 二氯甲烷 用作溶剂,化学反应生成4-甲氧基-1-萘甲醛 参考文献:Evaluation Of Synthetic Naphthalene Derivatives As Novel Chemical Chaperones That Mimic 4-Phenylbutyric Acid 标题:Evaluation Of Synthetic Naphthalene Derivatives As Novel Chemical Chaperones That Mimic 4-Phenylbutyric Acid 摘要:The Chemical Chaperone 4-Phenylbutyric Acid (4-Pba) Has Potential As An Agent For The Treatment Of Neurodegenerative Diseases. However,The Requirement Of High Concentrations Warrants Chemical Optimization For Clinical Use. In This Study,Novel Naphthalene Derivatives With A Greater Chemical Chaperone Activity Than 4-Pba Were Synthesized With Analogy To The Benzene Ring. All Novel Compounds Showed Chemical Chaperone Activity,And 2 And 5 Possessed High Activity. In Subsequent Experiments,The Protective Effects Of The Compounds Were Examined In Parkinson'S Disease Model Cells,And Low Toxicity Of 9 And 11 Was Related To Amphiphilic Substitution With Naphthalene. (C) 2015 Elsevier Ltd. All Rights Reserved. Doi:10.1016/j.Bmcl.2014.12.080
专利号:WO-2004031133-A1 优先权日:2002-10-04 标 题:Process for the synthesis of guanidine derivatives 发明人:EISENHUTH LUDWIG 权利人:FLEXSYS BV; EISENHUTH LUDWIG 摘要:The invention pertains to a process for the synthesis of guanidine derivatives of Formula (I) wherein X is selected from OH, OM wherein M is an alkali or earth alkali metal ion, and NR1R2 wherein R1 and R2 are independently H, C1-C6 alkyl, C2-C6 alkenyl, C3-C6 cycloalkyl, or C6-C10 aryl; which comprises a first step of reacting cyanogen chloride (N≡CCI) with NH3 in an organic solvent followed by a second step of reacting with an amine of Formula (II) wherein X has the previously given meaning, optionally followed by a step of converting a compound of Formula (I) into another compound of Formula (I).
专利号:US-6121054-A 优先权日:1997-11-19 标 题 :Method for separation of liquid and solid phases for solid phase organic syntheses 发明人:LEBL MICHAL 权利人:TREGA BIOSCIENCES INC 摘要:A simple, efficient apparatus and method for separation of solid and liquid phases useful in methods of high-throughput combinatorial organic synthesis of large libraries or megaarrays of organic compounds is disclosed. The apparatus and method are useful, whether as part of an automated, robotic or manual system for combinatorial organic synthesis. In a preferred embodiment, an apparatus and method of removal of liquid phase from solid phase compatible with microtiter plate type array(s) of reaction vessels is disclosed.
专利号:US-5175302-A 优先权日:1987-07-13 标 题 :Nucleophilic fluoroalkylation of aldehydes 发明人:STAHLY G PATRICK 权利人:ETHYL CORP 摘要:Aryl difluoromethyl sulfone adds to aldehydes under phase transfer conditions to give novel substituted alcohols of the general formula n n RCH(OH)CF.sub.2 SO.sub.2 Ar (I) n n wherein R is an aryl, cycloaliphatic, sec- or tert-aliphatic, or heterocyclic group and Ar is an aryl group. The substituted alcohols of formula I are of particular utility as intermediates in the synthesis of a variety of useful end products. For example, the products of formula I may be utilized in desulfonylation reactions, oxidation reactions and fluorination reactions.
专利号:US-4837327-A 优先权日:1987-07-13 标 题 :Process for nucleophilic fluoroalkylation of aldehydes 发明人:STAHLY G PATRICK 权利人:ETHYL CORP 摘要:Aryl difluoromethyl sulfone adds to alkehydes under phase transfer conditions to give novel substituted alcohols of the general formula n n RCH(OH)CF.sub.2 SO.sub.2 Ar (I) n n wherein R is an aryl, cycloaliphatic, sec- or tert-aliphatic, or heterocyclic group and Ar is an aryl group. The substituted alcohols of formula I are of particular utility as intermediates in the synthesis of a variety of useful end products. For example, the products of formula I may be utilized in desulfonylation reactions, oxidation reactions and fluorination reactions.
专利号:US-4999429-A 优先权日:1989-01-09 标 题 :Process for the preparation of α,α,β-1-trifluoro-1-olefinic derivatives 发明人:STAHLY G PATRICK 权利人:ETHYL CORP 摘要:Aryl difluoromethyl sulfone adds to aldehydes under phase transfer conditions to give novel substituted alcohols of the general formula n n RCH(OH)CF.sub.2 SO.sub.2 Ar (I) n n wherein R is an aryl, cycloaliphatic, sec- or tert-aliphatic, or heterocyclic group and Ar is an aryl group. The substituted alcohols of formula I are of particular utility as intermediates in the synthesis of a variety of useful end products. For example, the products of formula I may be utilized in desulfonylation reactions, oxidation reactions and fluorination reactions.
专利号:US-7056348-B2 优先权日:2001-04-19 标题:5-aryl-1,3,3-trimethyl-2-methylene-indoline derivatives and salts thereof, methods for the production and use of said compounds for the temporary coloration of fibers 发明人:SAUTER GUIDO; BRAUN HANS-JUERGEN; REICHLIN NADIA 权利人:WELLA AG 摘要:A method for the synthesis of 5-aryl-1,3,3,-trimethyl-2-methylene-indoline derivatives of Formula (I) or its salts of Formula (Ia) wherein 1 mole of a 5-aryl-2,3,3-trimethyl-3H-indole derivative of Formula (VII) is reacted for 1 to 44 hours at a temperature of 20° to 180° C. in an apolar, aprotic or polar, protic or polar aprotic solvent with 1 to 50 moles of a compound of Formula R1-A; new compounds of Formulas (I)/(Ia) and (V), obtainable by this method as well as an agent containing at least one compound of Formula (I)/(Ia) and a carbonyl/imine compound for dyeing keratinic fibers and a method for temporarily dyeing keratin fibers, for which the keratin fiber is dyed with the aforementioned agent and the dyeing, so obtained, is removed again at any later time by a sulfite preparation.
参考标题:Synthesis Of Flavokawain Analogues And Their Anti-Neoplastic Effects On Drug-Resistant Cancer Cells Through Hsp90 Inhibition 作者:Young Ho Seo,Sun You Park |发布日期:2014.4.20 摘要:Hsp90 Is An Ubiquitous Molecular Chaperone Protein, Which Plays An Important Role In Regulating Maturation And Stabilization Of Many Oncogenic Proteins. Due To Its Potential To Simultaneously Disable Multiple Signaling Pathways, Hsp90 Represents Great Promise As A Therapeutic Target Of Cancer. In This Study, We Synthesized Flavokawain Analogues And Evaluated Their Biological Activities Against Drug-Resistant Cancer Cells. The Study Indicated That Compound 1I Impaired The Growth Of Gefitinib-Resistant Non-Small Cell Lung Cancer (H1975), Down-Regulated The Expression Of Hsp90 Client Proteins Including Egfr, Her2, Met, Akt And Cdk4, And Upregulated The Expression Of Hsp70. The Result Strongly Suggested That Compound 1I Inhibited The Proliferation Of Cancer Cells Through Hsp90 Inhibition. Overall, Compound 1I Could Serve As A Potential Lead Compound To Overcome The Drug Resistance In Cancer Chemotherapy.
合成参考文献
摘要:S109 | PARCEDC | List of 7074 potential endocrine disrupting compounds (EDCs) by PARC T4.2 | DOI:10.5281/zenodo.10944198 摘要:Xiao, X., Science of Synthesis: Knowledge Updates, (2023) 2, 209. 参考文献:10.1023/a:1015871219922 摘要:Jelski W, Chrostek L, Szmitkowski M, Laszewicz W. Activity of Class I, II, III, and IV Alcohol Dehydrogenase Isoenzymes in Human Gastric Mucosa. Digestive Diseases and Sciences. 2002 Jul;47(7):1554–7. doi: 10.1023/a:1015871219922. 参考文献:10.1023/b:ddas.0000034557.23322.e0 摘要:Jelski W, Zalewski B, Chrostek L, Szmitkowski M. The Activity of Class I, II, III, and IV Alcohol Dehydrogenase Isoenzymes and Aldehyde Dehydrogenase in Colorectal Cancer. Digestive Diseases and Sciences. 2004 Jun;49(6):977–81. doi: 10.1023/b:ddas.0000034557.23322.e0.