3-氯-2-甲基乙酰苯胺置于盐酸,Potassium Permanganate,Magnesium Sulfate体系中,用 水 用作溶剂,化学反应 6.5H,反应生成2-氨基-6-氯苯甲酸 参考文献:Synthesis And Antitumor Evaluation Of Novel 5-Substituted-4-Hydroxy-8-Nitroquinazolines As Egfr Signaling-Targeted Inhibitors 标题:Synthesis And Antitumor Evaluation Of Novel 5-Substituted-4-Hydroxy-8-Nitroquinazolines As Egfr Signaling-Targeted Inhibitors 摘要:The Synthesis And Biological Activity Of A Series Of Novel 5-Substituted-4-Hydroxy-8-Nitroquinazolines That May Function As Inhibitors Of Egfr-And/or Erbb-2-Related Oncogenic Signaling Are Described. These Compounds Were Prepared By Snar Reaction Of 5-Chloro-4-Hydroxy-8-Nitroquinazo Line With Alkyl Or Aryl Amines,Or Alkyl Alcohol As Nucleophiles. Although The Enzyme Assay Showed A Weak Inhibition Effect Against Both Egfr And Erbb-2 Tyrosine Kinases,The Cell-Based Antitumor Activity Turned Out Promising. Compounds Having 5-Anilino Substituent Exhibit High Potency With 5-(4-Methoxy)Anilino-4-Hydroxy-8-Nitroquinazoline (1H) Being The Best Dual Egfr/erbb-2 Inhibitors,Which Effectively Inhibited The Growth Of Both Egfr (Mda-Mb-468,Ic50 < 0-01 Mu M) And Erbb-2 (Sk-Br-3,Ic50 = 13 Mu M) Overexpressing Human Tumor Cell Lines In Vitro. More Interestingly,The Variation Of The Substituent(S) At The 3-And/or 4-Position Of The 5-Anilino Portion Was Found To Modulate The Selectivity And Potency Dramatically. However,Compounds Having An Alkylamino Or Alkyloxy Group At The 5-Position Of 4-Hydroxy-8-Nitroquinazolines Are Essentially Inactive. These Results Are Consistent With Molecular Modeling Observations. This Study Was The First Attempt To Identify New Structural Types Of Dual Egfr/erbb-2-Related Signaling Inhibitors By Incorporation Of The Anilino Group At The 5-Position Of 4-Hydroxy-8-Nitroquinazolines' Core Structure,Providing Promising New Templates For Further Development Of Potent Inhibitors Targeting Both Egfr And Erbb-2 Tyrosine Kinases. (C) 2005 Elsevier Ltd. All Rights Reserved. Doi:10.1016/j.Bmc.2005.05.045
专利号:US-4154745-A 优先权日:1977-05-02 标题:Isobenzofuran route to anthracycloquinones 发明人:KENDE ANDREW S; TSAY YUH-GENG 权利人:RESEARCH CORP 摘要:There is provided a novel method of synthesizing certain tetracyclic quinones. In particular, there is provided a novel route to the synthesis of (±)-7-deoxydaunomycinone and analogs thereof which includes the provision of novel tetrahydronaphthoquinones and tetracyclic quinone intermediates. The compounds of the present invention are provided through a route comprising a Diels-Alder addition of certain isobenzofurans to certain novel tetrahydronaphthoquinones. The products of the synthetic route provided herein may be converted into compounds of known antibiotic and antineoplastic activity.
专利号:US-5925647-A 优先权日:1995-06-07 标 题 :Methods for use of cryptolepine analogs with hypoglycemic activity 发明人:BIERER DONALD E 权利人:SHAMAN PHARMACEUTICALS INC 摘要:Novel cryptolepine analogs useful as hypoglycemic agents and methods for their use as hypoglycemic agents, for example, in the treatment of diabetes, and a method for their synthesis are described. As hypoglycemic agents, the novel cryptolepine analogs are useful for the treatment of insulin-dependent diabetes mellitus (IDDM or Type I) and non-insulin dependent diabetes mellitus (NIDDM or Type II).
专利号:US-2015315143-A1 优先权日:2014-05-01 标题 :N-Heterocyclic Carbene-Catalyzed Synthesis of 2-Aryl Indoles
专利号:US-9527812-B2 优先权日:2014-05-01 标题 :N-heterocyclic carbene-catalyzed synthesis of 2-aryl indoles 发明人:SCHEIDT KARL A; HOVEY JR MICHAEL TODD; CHECK CHRISTOPHER 权利人:UNIV NORTHWESTERN 摘要:Transition metal-free catalytic methods for access to 2-arylindole compounds.
专利号:RU-2163240-C2 优先权日:1994-11-02 标题 :Derivatives of substituted tetracyclic azepine, method of their synthesis, pharmaceutical composition, intermediate substance and method of its synthesis
专利号:US-9992996-B2 优先权日:2007-09-28 标题 :Bioactive aniline copolymers 发明人:GIZDAVIC-NIKOLAIDIS MARIJA; EASTEAL ALLAN J; STEPANOVIC SRDJAN 权利人:AUCKLAND UNISERVICES LTD 摘要:Aniline copolymers and the synthesis thereof for use as antimicrobial (antibacterial, antifungal or antiviral material) material of for the manufacture of antimicrobial objects, suitable for use in the health, food, packaging, water, paint, wood, textile, poultry, glass, paper, rubber, ceramic, seafood, sports, plastic and agricultural industries. The copolymer may be for example (A): where for example R 3 â•?H 5 —CO 2 H, —CO 2 Me, or —CO 2 Et. R is typically H or a C 1 -C 6 alkyl, x is an integer between 1 and 0 and m indicates the degree of polymerization. Preferred copolymers are copolymers of aniline with 3-aminobenzoic acid, 2-aminobenzoic acid and ethyl 3-aminobenzoate.
参考文献:10.1186/1475-2859-5-1 摘要:Retallack DM, Thomas TC, Shao Y, Haney KL, Resnick SM, Lee VD, Squires CH. Identification of anthranilate and benzoate metabolic operons of Pseudomonas fluorescens and functional characterization of their promoter regions. Microbial Cell Factories. 2006 Jan 05;5(1):1. doi: 10.1186/1475-2859-5-1.