4-羟基-1-哌啶甲酸苄酯置于palladium On Activated Charcoal,乙二胺 氢气,Silica Gel,Pyridinium Chlorochromate体系中,用 四氢呋喃,甲醇,二氯甲烷 作为反应溶剂,20.0 °C,101.33 Kpa 条件下,反应 47.75H,反应生成 4-哌啶乙酸乙酯 参考文献:Pd/c(En)-Catalyzed Chemoselective Hydrogenation With Retention Of The N-Cbz Protective Group And Its Scope And Limitations 标题:Pd/c(En)-Catalyzed Chemoselective Hydrogenation With Retention Of The N-Cbz Protective Group And Its Scope And Limitations 摘要:A Chemoselective Method For The Hydrogenation Of Acetylene,Olefin,Azide,Nitro And Benzyl Ester Functionalities With Retention Of The Aliphatic N-Cbz Group Was Established. The Chemoselectivity Was Accomplished By Using A Combination Of 5% Pd/c-Ethylenediamine [5% Pd/c(En)] And Thf (Or 1,4-Dioxane) As A Solvent,And The Scope And Limitations Of This Methodology Were Investigated. These Results Reinforce The Utility Of N-Cbz Protective Groups In Synthetic Chemistry,Especially In Peptide Synthesis (C) 2000 Elsevier Science Ltd. All Lights Reserved. DOI:10.1016/s0040-4020(00)00771-7
专利号:WO-2021018023-A1 优先权日:2019-08-01 标题:Small molecule glp-1 receptor modulator 发明人:XIE FANG; YU GUANGXIA; ZHANG SHUJUAN 权利人:THE TITAN LEADING MED TECH INC 摘要:The present invention provides a new compound for modulating a Glucagon-like peptide-1 (GLP-1) receptor, and a synthesis method therefor and a pharmaceutical use thereof. This kind of compound has an obvious agonistic effect on the GLP-1 receptor, but does not have an obvious binding effect on hERG, and therefore, it is indicated that the compound has a low risk of cardiotoxicity. The compound of the present invention can be used alone as a treatment medication for type II diabetes, or be used in combination with a polypeptide GLP-1 receptor agonist such as liraglutide, or be used in combination with the treatment medication for type II diabetes of other mechanisms.
专利号:US-2014315915-A1 优先权日:2009-02-09 标题:Design, synthesis and evaluation of procaspase activating compounds as personalized anti-cancer drugs
专利号:US-9522901-B2 优先权日:2005-05-26 标题:Compositions and methods including cell death inducers and procaspase activation 发明人:HERGENROTHER PAUL J; PUTT KARSON S; PETERSON QUINN P; FAKO VALERIE 权利人:UNIV ILLINOIS 摘要:Compositions and methods are disclosed in embodiments relating to induction of cell death such as in cancer cells. Compounds and related methods for synthesis and use thereof, including the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells are disclosed. Compounds are disclosed in connection with modification of procaspases such as procaspase-3. In embodiments, compositions are capable of activation of procaspase-3.
专利号:RU-2156765-C2 优先权日:1994-08-19 标 题:Derivatives of oxazolidinone carboxylic acid, method of their synthesis, pharmaceutical composition
专利号:US-2012040995-A1 优先权日:2009-02-09 标 题:Design, synthesis and evaluation of procaspase activating compounds as personalized anti-cancer drugs
专利号:US-9102661-B2 优先权日:2009-02-09 标题:Design, synthesis and evaluation of procaspase activating compounds as personalized anti-cancer drugs
参考文献:10.1055/s-2008-1072717 摘要:Taddei M, Piras L, Genesio E, Ghiron C. Microwave-Assisted Hydrogenation of Pyridines. Synlett. 2008 May;2008(8):1125–8. doi: 10.1055/s-2008-1072717.