N,N'-二-Boc-1,4-丁二胺置于甲酸,N,N'-二异丙基碳二亚胺体系中,用 二氯甲烷 作为反应溶剂,化学反应生成 N-叔丁氧羰基-1,4-丁二胺 参考文献:Improved Synthesis Of 15-Deoxyspergualin Analogs Using The Ugi Multi-Component Reaction 标题:Improved Synthesis Of 15-Deoxyspergualin Analogs Using The Ugi Multi-Component Reaction 摘要:Spergualin Is A Natural Product That Exhibits Immunosuppressive,Anti-Tumor And Anti-Bacterial Activities. Its Derivatives,Such As 15-Deoxyspergualin (15-Dsg),Have Been Clinically Approved For Acute Allograft Rejection. However,The Reported Syntheses Are Cumbersome (>10 Steps) And They Suffer From Low Overall Yields (Similar To 0.3% To 18%). Moreover,Spergualin And Its Derivatives Are Chemically Unstable And Rapidly Hydrolyzed In Aqueous Buffer. Here,We Have Re-Explored These Issues And Report A Modified Synthetic Route With Significantly Improved Overall Yield (Similar To 31% To 47%). The Key Transformation Is A Microwave-Accelerated Ugi Multi-Component Reaction That Is Used To Generate The Peptoid Core In A Single Step. Using The Products Of This Route,We Found That Modifications Of The Hemiaminal Significantly Increased Chemical Stability. Thus,We Anticipate That This Synthetic Route Will Improve Access To Biologically Active 15-Dsg Derivatives. (C) 2011 Elsevier Ltd. All Rights Reserved. DOI:10.1016/j.Bmcl.2011.02.079
专利号:US-7138526-B1 优先权日:1999-06-15 标 题 :Solid phase synthesis of n,n-disubstituted diazacycloalkylcarboxy derivatives 发明人:HERPIN TIMOTHY F; MORTON GEORGE C; SALVINO JOSEPH M 权利人:AVENTIS PHARMA INC 摘要:A method for the solid phase synthesis of N,N-disubstituted diazacycloalkylcarboxy derivatives of general formula (I) and (II) is claimed. Examples include piperazine-2-carboxamide. The method is applicable to the synthesis or large combinatorial libraries
专利号:US-2025129021-A1 优先权日:2023-09-19 标 题:Small molecule protein synthesis modulators 发明人:GYGI DAVID; BAHMANYAR SOGOLE SAMI; HAMANN LAWRENCE 权利人:INTERDICT BIO INC 摘要:The present disclosure provides compounds of the formulae herein (e.g., Formula (I), Formula (V)), and pharmaceutically acceptable salts thereof, which are useful for modulating protein synthesis (e.g., modulating synthesis of BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D). The present disclosure also provides pharmaceutical compositions and kits comprising the compounds, or pharmaceutically acceptable salts thereof, and methods of treating or preventing diseases or disorders (e.g., diseases or disorders associated with BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D) by administering to a subject in need thereof the compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof.
专利号:US-2009099061-A1 优先权日:2006-01-27 标 题:Synthesis of carotenoid analogs or derivatives with improved antioxidant characteristics 发明人:FOSS BENTE J; NADOLSKI GEOFFRY T; LOCKWOOD SAMUEL F 权利人:FOSS BENTE J; NADOLSKI GEOFFRY T; LOCKWOOD SAMUEL F 摘要:A method is described for synthesizing and administering carotenoid compounds with improved antioxidant characteristics. In some embodiments, extension or improvement of conjugation may be employed in structural modification of carotenoids. In other embodiments, reduction of ring/chain steric hindrance may improve the lambda max, and hence, the overall antioxidant capability, of particular compounds. In other embodiments, introduction and/or increase in synthetic handles for conjugation may improve the stoichiometric ratios of conjugating moieties to the polyene backbone. The methods may be used to improve natural and/or synthetic compounds for medicinal application in the treatment of disease.
专利号:US-2023219881-A1 优先权日:2022-01-11 标题 :Synthesis of Spermidine, Spermine, and Free Bases Thereof 发明人:TITLOW MATTHEW; GU XINGLONG 权利人:COMPOUND SOLUTIONS INC; SHAOXING KING YEAR BIOCHEMICAL CO LTD 摘要:A simplified synthetic process for production of spermine and spermidine are presented that can provide spermine and spermidine in free base or salt form. Advantageously, the synthetic procedure is safe, simple, and environmentally friendly, while at the same time also being cost-effective.
专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
专利号:US-2021299285-A1 优先权日:2018-07-17 标题 :Compounds useful for in vivo imaging of protein oxidation and/or cancer treatment 发明人:FURDUI CRISTINA M; POOLE LESLIE B; KING S BRUCE 权利人:UNIV WAKE FOREST HEALTH SCIENCES 摘要:Provided herein are compounds of Formula I, Formula II Formula III which are useful in labeling tissues in a subject (e.g., PET imaging of a subject), for treatment of cancer, and/or for preparing a medicament. Also provided are compounds containing a group that is reactive with sulfenylated proteins for treatment of cancer and/or for preparing a medicament. Methods of synthesis of the compounds and precursor compounds are also provided.
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合成参考文献
摘要:Tomás-Gamasa, M., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 14. 参考文献:10.1007/s11307-019-01365-y 摘要:Zhang A, Wu T, Bian L, Li P, Liu Q, Zhang D, Jin Q, Zhang J, Huang G, Song S. Synthesis and Evaluation of Ga-68-Labeled Rhein for Early Assessment of Treatment-Induced Tumor Necrosis. Molecular Imaging and Biology. 2019 Jun 27;22(3):515–25. doi: 10.1007/s11307-019-01365-y.