CAS: 254750-02-2; (S)-3-((S)-2-(2-((2-(Tert-Butyl)Phenyl)Amino)-2-Oxoacetamido)Propanamido)-4-Oxo-5-(2,3,5,6-Tetrafluorophenoxy)Pentanoic Acid

上下游产品

(S)-2-(2-((2-(叔丁基)苯基)氨基)-2-氧代乙酰氨基)丙酰氨基)-4-氧代-5-( (3S)-3-[n-(N'-(2-Tert-Butylphenyl)Oxamyl)Alaninyl]Amino-5-(2',3',5',6'-Tetrafluorophenoxy)-4-Oxopentanoic Acid Tert-Butyl Ester 254750-83-9

📜N-Pyruvoyl-L-Alanin-Methylester置于chromium(Vi) Oxide,草酰氯,甲基叔丁基醚,水,氯乙酰氯,三氟乙酸,N,N-二乙基苯胺,Sodium Hydroxide,三甲胺体系中,用 甲醇,二氯甲烷,氯仿,水,乙腈,正丁醇 用作溶剂,化学反应 24.0H,反应生成恩利卡生
参考文献:一种恩利卡生的合成方法
标题:一种恩利卡生的合成方法
摘要:一种恩利卡生的合成方法,属于药物化学合成技术领域.步骤:先由丙酮酸与酰氯化试剂进行酰氯化反应,得到丙酮酰氯,再将丙酮酰氯和l‑丙氨酸甲酯进行缩合反应,得到中间体(i);将中间体(i)进行水解反应,得到羧酸衍生物,将羧酸衍生物与酰氯化试剂进行酰氯化反应,得到酰氯衍生物,再将该酰氯衍生物进行缩合反应,得到中间体(II);将中间体(II)进行氧化反应,得到羧酸衍生物,将该羧酸衍生物与酰氯化试剂进行酰氯化反应,得到酰氯衍生物,再将酰氯衍生物进行缩合反应,得到叔丁酯衍生物,再将该叔丁酯衍生物用三氟乙酸处理,进行水解反应,得到成品恩利卡生.简化操作,每一步都能获得较高的收率;满足工业化放大生产要求.

专利信息

专利号:US-2024400552-A1
优先权日:2016-11-11
标题 :Heterocyclic modulators of lipid synthesis
发明人：BUCKLEY DOUGLAS I; DUKE GREGORY; WAGMAN ALLAN S; EVANCHIK MARC; MCDOWELL ROBERT S
权利人:SAGIMET BIOSCIENCES INC
摘要:Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by dysregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders, such as non-alcoholic steatohepatitis (NASH).

专利号:US-11622968-B2
优先权日:2011-03-08
标 题:Heterocyclic modulators of lipid synthesis
发明人：BUCKLEY DOUGLAS; DUKE GREGORY; WAGMAN ALLAN S; EVANCHIK MARC; MCDOWELL ROBERT S
权利人:SAGIMET BIOSCIENCES INC
摘要:Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by disregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders, such as non-alcoholic steatohepatitis (NASH).

专利号:US-12358903-B2
优先权日:2016-06-13
标题 :FXR (NR1H4) modulating compounds
发明人：BLOMGREN PETER A; CURRIE KEVIN S; FARAND JULIE; GEGE CHRISTIAN; KROPF JEFFREY E; XU JIANJUN
权利人:GILEAD SCIENCES INC
摘要:The present disclosure relates generally to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.

专利号:US-11739065-B2
优先权日:2016-06-13
标题 :FXR (NR1H4) modulating compounds
发明人：BLOMGREN PETER A; CURRIE KEVIN S; GEGE CHRISTIAN; KROPF JEFFREY E; XU JIANJUN
权利人:GILEAD SCIENCES INC
摘要:The present disclosure relates generally to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.

专利号:US-2024208898-A1
优先权日:2021-03-25
标 题 :Enamine n-oxides: synthesis and application to hypoxia-responsive prodrugs and imaging agents
发明人：KIM JUSTIN; KANG DAHYE; CHEUNG SHELDON T
权利人:DANA FARBER CANCER INST INC
摘要:Disclosed are compounds and pharmaceutically acceptable salts and stereoisomers thereof that are suitable for diagnosis and the treatment of diseases and disorders characterized by, associate with or which exhibit tissue hypoxia, such as, for example, solid tumors. Also disclosed are pharmaceutical compositions containing same, and methods of making and using the compounds.

专利号:US-11285169-B2
优先权日:2013-03-13
标题 :Methods for modulating chemotherapeutic cytotoxicity
发明人：ROBERTS DAVID D; SOTO PANTOJA DAVID R
权利人:US HEALTH
摘要:Methods of reducing cytotoxicity of a chemotherapeutic agent to non-cancer cells by administering to a subject with cancer an effective amount of an agent that inhibits CD47 signaling and a DNA damaging agent, such as an anthracycline, topoisomerase inhibitor, or nucleotide synthesis inhibitor, are provided. Example disclosed methods reduce cardiotoxicity. In one example, the methods include administering to a subject with cancer an effective amount of a CD47 antisense morpholino oligonucleotide and an anthracycline such as doxorubicin. Methods of increasing cytotoxicity of a chemotherapeutic agent in cancer cells by administering to a subject with a tumor an effective amount of an agent that inhibits CD47 signaling and a DNA damaging agent such as an anthracycline, topoisomerase inhibitor, or nucleotide synthesis inhibitor, are also provided. In some embodiments, the inhibitor of CD47 signaling is administered to the subject before, during, or after the administration of the DNA damaging agent.