CAS: 3094-09-5; 1-((2R,3R,4S,5R)-3,4-Dihydroxy-5-Methyltetrahydrofuran-2-yl)-5-Fluoropyrimidine-2,4(1H,3H)-Dione

相似化合物

3094-09-5 316-46-1 15958-99-3

上下游产品

5-氟尿嘧啶核苷 5-Fluorouridine 316-46-1
5'-Deoxy-5'-Iodo-5-Fluorouridine 61787-13-1
5'-脱氧尿苷 5'-Deoxyuridine 15958-99-3
5'-脱氧-5-氟-2',3'-O-异亚丙基尿苷 5′-Deoxy-2′,3′-O-Isopropylidene-5-Fluorouridine 66335-39-5
2',3'-Di-O-Benzoyl-5'-Deoxy-5-Fluorouridine 77180-87-1
加洛他滨 5'-Deoxy-5-Fluoro-N4-(3,4,5-Trimethoxybenzoyl)Cytidine 124012-42-6

2',3'-Di-O-Benzoyl-5'-Deoxy-5-Fluorouridine置于sodium Methylate体系中,用 甲醇 作为反应溶剂,化学反应生成 去氧氟尿苷
参考文献:Preparation,Antibacterial Effects And Enzymatic Degradation Of 5-Fluorouracil Nucleosides
标题:Preparation,Antibacterial Effects And Enzymatic Degradation Of 5-Fluorouracil Nucleosides
摘要:在冰乙酸中,尿嘧啶的苄酰化醛基五糖衍生物与氟反应反应生成了苄酰化的5-氟尿嘧啶核苷.它们的甲醇解产生了以下的游离5-氟尿嘧啶核苷:β-D-核糖呋喃苷(id),2-脱氧-β-D-核糖呋喃苷(iid),它们的对映异构体viii和ix,α-D-核糖呋喃苷(xiii),2-脱氧-α-D-核糖呋喃苷(xv),β-D-阿拉伯呋喃苷(iv)及其l-对映体x,β-D-木糖呋喃苷(v)及其α-D-异构体xi,α-L-吕糖呋喃苷(vi)和2-脱氧-α-L-吕糖呋喃苷(vii)以及后两种化合物的对映体xii和xiv.类似地获得了5-脱氧-β-D-核糖呋喃苷(iii),β-D-核糖吡喃苷(xvi)和1-(S)-(2,3-二羟基丙基)-5-氟尿嘧啶(xviic).1-丙烯基-5-氟尿嘧啶(xviii)是通过丙烯基溴和2,4-双(三甲基硅氧基)-5-氟嘧啶反应制备的.大肠杆菌的细胞提取物可裂解所有5-氟尿嘧啶核苷,其中核苷碳原子具有r-构型,糖基的3'-羟基与碱基呈反式关系.不具备这些结构特征的化合物是抗性的.除了在酶解时产生5-氟尿嘧啶的核苷外,还有不可裂解的1-(2-脱氧-β-L-核糖呋喃基)-5-氟尿嘧啶(ix),1-(2-脱氧-α-D-核糖呋喃苷)-5-氟尿嘧啶(xv)和1-(2-脱氧-α-D-吕糖呋喃苷)-5-氟尿嘧啶(xiv)对大肠杆菌表现出抗菌作用(id50为1.0-2.5 X 10^-5 M).这种效应可以被2'-脱氧尿苷而不是胸苷逆转.
DOI:10.1135/cccc19803217

专利信息

专利号:US-12383499-B2
优先权日:2018-01-01
标题:Scale up synthesis of silicasome nanocarriers
发明人：NEL ANDRE E; MENG HUAN; LIU XIANGSHENG
权利人:UNIV CALIFORNIA
摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).

专利号:US-10925977-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
发明人：YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

专利号:US-10973847-B2
优先权日:2017-06-30
标题 :Core-to-surface polymerization for the synthesis of star polymers and uses thereof
发明人：JOHNSON JEREMIAH A; GOLDER MATTHEW R
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:Disclosed are methods, compositions, reagents, systems, and kits to prepare star polymers, as well as compositions and uses thereof. Various embodiments show that synthesis of these polymers contain low metal concentration to provide polymers for diverse biomedical applications including in vivo applications.

专利号:US-12391691-B2
优先权日:2018-11-16
标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
发明人：PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
权利人:AMGEN INC
摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as

专利号:US-2025206736-A1
优先权日:2019-11-14
标题 :Synthesis of kras g12c inhibitor compound
发明人：CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN
权利人:AMGEN INC
摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.

专利号:WO-2017100796-A1
优先权日:2015-12-11
标 题 :Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
发明人：WONG CHI-HUEY; HSU TSUI-LING; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI
权利人:SINACA ACAD; WONG CHI-HUEY; HSU TSUI-LING
摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta- 4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for disgnostic and therapeutic uses.