865605-32-9 = 67385-09-5 + 89343-06-6 + 865605-35-2 反应条件:1.1 Catalysts: 1,1-Bis(Diphenylphosphino)Ferrocene,Hydrotetrakis(Triphenylphosphine)Rhodium Solvents: Acetone; 1 H,Reflux 标题:Equilibrating C-S Bond Formation By C-H And S-S Bond Metathesis. Rhodium-Catalyzed Alkylthiolation Reaction Of 1-Alkynes With Disulfides 作者:Arisawa,Mieko; Fujimoto,Kenji; Morinaka,Satoshi; Yamaguchi,Masahiko 参考文献:Journal Of The American Chemical Society 日期:2005 卷标:127(35) 页码:12226-12227
S-[2-({[(2-甲基-2-丙基)氧基]羰基}氨基)乙基]硫代乙酸酯置于sodium Methylate体系中,用 甲醇 作为反应溶剂,化学反应 0.25H,反应生成 2-叔丁氧羰基氨基乙硫醇 参考文献:Constrained (L-)-S-Adenosyl-L-Homocysteine (Sah) Analogues As Dna Methyltransferase Inhibitors 标题:Constrained (L-)-S-Adenosyl-L-Homocysteine (Sah) Analogues As Dna Methyltransferase Inhibitors 摘要:Potent Sah Analogues With Constrained Homocysteine Units Have Been Designed And Synthesized As Inhibitors Of Human Dnmt Enzymes. The Five Membered (2S,4S)-4-Mercaptopyrrolidine-2-Carboxylic Acid,In 1A,Was A Good Replacement For Homocysteine,While The Corresponding Six-Member Counterpart Was Less Active. Further Optimization Of 1A,Changed The Selectivity Pro. Le Of These Inhibitors. A Chloro Substituent At The 2-Position Of 1A,Compound 1D,Retained Potency Against Dnmt1,While N-6 Alkylation,Compound 7A,Conserved Dnmt3B2 Activity. The Concomitant Substitutions Of 1A At Both 2-And N-6 Positions Reduced Activity Against Both Enzymes. (C) 2009 Elsevier Ltd. All Rights Reserved. DOI:10.1016/j.Bmcl.2009.03.132
专利号:US-10370409-B2 优先权日:2011-10-25 标题 :Synthesis of libraries of peptide tertiary amides 发明人:KODADEK THOMAS; GAO YU 权利人:SCRIPPS RESEARCH INST 摘要:The present disclosure is directed to a novel class of peptide-like oligomers called peptide tertiary amides (PTAs) and a combinatorial library of PTAs along with synthetic routes for the preparation of large combinatorial libraries of these compounds. The peptide tertiary amides provide an exceptional source of high affinity and selective protein ligands that are useful as tools for biological research and as drug leads, among others.
专利号:US-11918657-B2 优先权日:2017-11-10 标 题 :Dendrimer delivery system and methods of use thereof 发明人:RANGARAMANUJAM KANNAN; SHARMA RISHI; SHARMA ANJALI; KANNAN SUJATHA; ZHANG ZHI; KAMBHAMPATI SIVA PRAMODH 权利人:UNIV JOHNS HOPKINS 摘要:Low-generation dendrimers containing a high density of surface hydroxyl groups, and methods of synthesis thereof are provided. In particular, oligo ethylene glycol (OEG)-like dendrimers with a high surface functional groups at relatively low generations (e.g. Ëœ120 hydroxyls in the third generation, with a size of just 1-2 nm) is described. Dendrimer formulations including one or more prophylactic, therapeutic, and/or diagnostic agents, and methods of use thereof are also described. The formulations are suitable for topical, enteral, and/or parenteral delivery for treating one or more diseases, conditions, and injuries in the eye, the brain and nervous system (CNS), particularly those associated with pathological activation of microglia and astrocytes.
专利号:US-2014315831-A1 优先权日:2011-10-25 标 题:Synthesis of Libraries of Peptide Tertiary Amides
专利号:US-11279734-B2 优先权日:2017-12-01 标 题:Solution-phase affinity selection of inhibitors from combinatorial peptide libraries 发明人:PENTELUTE BRADLEY L; TOUTI FAYCAL 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:The present invention provides novel peptides (e.g., peptides, macrocyclic peptides, mini-proteins) that modulate protein-protein interactions or salts thereof, and methods of making and using the inventive peptides. In some embodiments, the peptides are high affinity inhibitors (e.g., K D of at most 100 nM, at most 10 nM, at most 1 nM) of a protein-protein interaction. In certain embodiments, these peptides interfere with p53-MDM2 binding interactions (e.g., by binding to MDM2 (GenBank® Gene ID: 4193)). In some embodiments, the peptides interfere with the dimerization of the C-terminal domain of the human immunodeficiency virus (HIV) capsid protein (C-CA), comprising residues 146-231 of the HIV capsid protein (e.g., by binding to the C-terminal domain of the HIV capsid protein (C-CA), thereby inhibiting the dimeric interface of HIV capsid protein, thereby inhibiting viral assembly). These inventive peptides were rapidly generated and identified using novel methods described herein comprising combinatorial peptide synthesis and/or solution affinity selection.
专利号:WO-2013063296-A1 优先权日:2011-10-25 标题 :Synthesis of libraries of peptide tertiary amides
专利号:US-9241917-B2 优先权日:2003-03-17 标 题 :Facially amphiphilic polymers and oligomers and uses thereof 发明人:DEGRADO WILLIAM F; TEW GREGORY N; KLEIN MICHAEL L; LIU DAHUI; YUAN JING; CHOI SUNGWOOK 权利人:DEGRADO WILLIAM F; TEW GREGORY N; KLEIN MICHAEL L; LIU DAHUI; YUAN JING; CHOI SUNGWOOK; UNIV PENNSYLVANIA 摘要:The present invention discloses methods of use of facially amphiphilic polymers and oligomers, including pharmaceutical uses of the polymers and oligomers as antimicrobial agents and antidotes for hemorrhagic complications associated with heparin therapy. The present invention also discloses novel facially amphiphilic polymers and oligomers and their compositions, including pharmaceutical compositions. The present invention further discloses the design and synthesis of facially amphiphilic polymers and oligomers.
参考标题:Metal-Free Thioesterification Of Amides Generating Acyl Thioesters 作者:Qun Wang,Long Liu,Jianyu Dong,Zhibin Tian,Tieqiao Chen 摘要:A Base-Initiated Thioesterification Of Amides With Various Thiols Is Reported. This Reaction Can Take Place Efficiently Under Metal-Free And Air-Atmospheric Conditions, And Provides A Facile And Practically Useful Approach To The Synthesis Of Valuable Acyl Thioesters.
合成参考文献
摘要:Cellnik, T.; Jo, W.; Healy, A., Science of Synthesis: Knowledge Updates, (2024) 2, 385.