4-(Boc-氨基)-3-碘吡啶置于高氯酸四乙基铵,三乙胺体系中,用 乙醇,二甲基亚砜 作为反应溶剂,化学反应 10.0H,以86%的收率获得产物4-(叔丁氧羰基氨基)吡啶 参考文献:A Facile And Versatile Electro-Reductive System For Hydrodefunctionalization Under Ambient Conditions 标题:A Facile And Versatile Electro-Reductive System For Hydrodefunctionalization Under Ambient Conditions 摘要:描述了一种使用三乙胺作为牺牲还原剂的简便电还原去功能化系统,通过简单地改变反应溶剂,可以方便地切换还原的选择性和能力. DOI:10.1039/d1Gc00317H
专利号:US-5681959-A 优先权日:1995-02-21 标题:Chemical synthesis of azaindoles 发明人:BISHOP BRIAN CCHRISTOPHER; COTTRELL IAN FRANK; CAMERON MARK; HANDS DAVID 权利人:MERCK SHARP & DOHME 摘要:The present invention relates to a process for the preparation of azaindole derivatives of the formula ##STR1## wherein Q is hydrogen, C 1-6 alkyl, C 2-6 alkenyl, C 1-6 alkoxy, hydroxy, aryl or arylC 1-4 alkyl; n one of X, Y and Z is --Nâ•? and the others are --CHâ•?; n R 1 is hydrogen, C 1-6 alkyl, C 2-6 alkenyl or C 1-6 alkyl substituted by a group selected from aryl or --NR 2 R 3 where R 2 and R 3 each independently represent C 1-4 alkyl, or R 2 and R 3 , together with the nitrogen atom to which they are attached, form a 4-7 membered saturated heterocyclic ring, optionally containing in the ring an oxygen or sulphur atom or a group NR 4 where R 4 is C 1-4 alkyl, aryl or arylC 1-4 alkyl; and n R 5 is a hydrogen atom or a group selected from C 1-6 alkyl or aryl.
专利号:US-2007299102-A1 优先权日:2004-04-08 标题:Diphenyl Ox-Indol-2-One Compounds and Their Use in the Treatment of Cancer 发明人:FELDING JAKOB; PEDERSEN HANS C; KROG-JENSEN CHRISTIAN; PRAESTEGAARD MORTEN; BUTCHER STEVEN P; LINDE VIGGO; COULTER THOMAS S; MONTALBETTI CHRISTIAN; UDDIN MOHAMMED; REIGNIER SERGE 权利人:TOPOTARGET AS 摘要:The present invention relates to substituted 3,3-diphenyl-1,3-dihydro-indol-2-one compounds, and the use of such compounds for the preparation of a medicament for the treatment of cancer in a mammal. It is postulated that treatment of cancers is achieved in which inhibition of protein synthesis and/or inhibition of activation of the mTOR pathway is an effective method for reducing cell growth. Examples of such cancers are breast cancer, renal cancer, multiple myeloma, leukemia, glia blastoma, rhabdomyosarcoma, prostate, soft tissue sarcoma, colorectal sarcoma, gastric carcinoma, head and neck squamous cell carcinoma, uterine, cervical, melanoma, lymphoma, and pancreatic cancer. A particular subclass of compounds are represented by the formula (II) n n nwherein at least one of X 1 and X 2 is a heteroatom substituent, e.g. 6-chloro-3,3-bis-(4-hydroxy-phenyl)-7-methyl-1,3-dihydro-indol-2-one.
专利号:GB-2298199-A 优先权日:1995-02-21 标题:Synthesis of azaindoles
参考文献:10.1055/s-0036-1588938|10.1055/s-0036-1589495 摘要:Bronner S, Lee D, Bacauanu V, Cyr P. A Novel Cascade Benzyne Nucleophilic Addition/Fries Rearrangement for Entry into 2,3-Disubstituted Phenols. Synlett. 2017 Jan 19;28(07):799–804. doi: 10.1055/s-0036-1588938. 参考文献:10.1055/s-0039-1690239 摘要:Mittal R, Mishra A, Awasthi SK. A Greener Approach for the Chemoselective Boc Protection of Amines Using Sulfonated Reduced Graphene Oxide as a Catalyst in Metal- and Solvent-Free Conditions. Synthesis. 2019 Nov 06;52(04):591–601. doi: 10.1055/s-0039-1690239.