CAS: 102195-80-2; (S)-1-Tert-Butyl 2-Methyl 4-Oxopyrrolidine-1,2-Dicarboxylate

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CAS号74844-91-0 N-B°C-反式-4-羟基-L... | CAS号79-37-8 草酰氯 | CAS号796095-60-8 (2S)-methyl 1-(... | CAS号67-68-5 二甲基亚砜 | CAS号13726-69-7 B°C-L-羟脯氨酸 | CAS号7529-22-8 N-甲基吗啉氧化物 | CAS号24424-99-5 二碳酸二叔丁酯 | CAS号1499-56-5 (2S,4R)-4-羟基吡咯烷... | CAS号51-35-4 L-羟脯氨酸 | CAS号40216-83-9 L-羟脯氨酸甲酯盐酸盐 | CAS号336818-78-1 (2S,4R)-N-叔丁氧羰基... | CAS号215918-21-1 (2S)-4,4-二氟-2-(... | CAS号487-79-6 海藻酸(mM/ml) | CAS号74844-93-2 B°C-4-去氢-L-脯氨酸 | CAS号1129634-44-1 (S)-5-(叔丁氧羰基)-5... | CAS号203866-17-5 N-B°C-4,4-二氟-L-脯氨酸甲酯 | CAS号203866-15-3 N-B°C-4,4-二氟-L-脯氨酸 | CAS号1129634-43-0 (S)-5-叔丁基-6-甲基5... | CAS号808154-66-7 L-Proline, 4-(d...

L-羟基脯氨酸置于氯化亚砜,三氧化硫吡啶,三乙胺体系中,用 二氯甲烷,二甲基亚砜 用作溶剂,化学反应 18.0H,反应生成Boc-4-氧代-L-脯氨酸甲酯
参考文献:γ-(S)-三氟甲基脯氨酸:评估为脯氨酸在固态(19)f-NMR肽研究中的结构替代物.
标题:γ-(S)-三氟甲基脯氨酸:评估为脯氨酸在固态(19)f-NMR肽研究中的结构替代物.
摘要:γ-(4S)-三氟甲基脯氨酸是根据改良的文献方法合成的,具有改进的收率(以克为单位).使用n-乙酰基甲基酯模型表征了由氨基酸形成的酰胺键的构象性质.发现异构化的酰胺族(s-反式对s-顺式)和热力学参数与完整脯氨酸的相应值相似.因此,对于通过(19)f-NMR进行结构研究,γ-三氟甲基脯氨酸被认为是肽中结构上低干扰的脯氨酸取代.确实,在肽抗生素短杆菌肽s中天然脯氨酸换成γ-三氟甲基脯氨酸被证明保留了整个两亲性肽结构.
Doi:10.1039/c5Ob00034C

专利信息

专利号:US-2012095211-A1
优先权日:2010-09-22
标 题 :Substituted proline inhibitors of hepatitis c virus replication
发明人：BUCKMAN BRAD; NICHOLAS JOHN B; SEREBRYANY VLADIMIR; SEIWERT SCOTT D
权利人:BUCKMAN BRAD; NICHOLAS JOHN B; SEREBRYANY VLADIMIR; SEIWERT SCOTT D; INTERMUNE INC
摘要:The embodiments provide compounds of the general Formulae I, Ia, II, IIa, III, IIIa, IIIb, IV, IVa, IVb, V, Va, Vb, VI, VIa, VIb, and VIc, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition. The embodiments also provide methods for the synthesis of subject compounds and intermediates in the synthetic methods.

专利号:US-9549921-B2
优先权日:2013-06-24
标 题:Heterocyclic compounds and methods of use thereof for the treatment of hepatitis C
发明人：HE SHUWEN; LAI ZHONG; DAI XING; XIAO DONG; LONDON CLARE; ZORN NICOLAS; NARGUND RAVI; PALANI ANANDAN; MCCOMAS CASEY C; LI PENG; PENG XUANJIA; SOLL RICHARD
权利人:HE SHUWEN; LAI ZHONG; DAI XING; XIAO DONG; LONDON CLARE; ZORN NICOLAS; NARGUND RAVI; PALANI ANANDAN; MCCOMAS CASEY C; LI PENG; PENG XUANJIA; SOLL RICHARD; MERCK SHARP & DOHME
摘要:The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.(I)

专利号:US-10906033-B2
优先权日:2016-03-28
标题 :Synthesis and application of chiral substituted polyvinylpyrrolidinones
发明人：HUA DUY H
权利人:UNIV KANSAS STATE
摘要:Chiral polyvinylpyrrolidinone (CSPVP), complexes of CSPVP with a core species, such as a metallic nanocluster catalyst, and enantioselective oxidation reactions utilizing such complexes are disclosed. The CSPVP complexes can be used in asymmetric oxidation of diols, enantioselective oxidation of alkenes, and carbon-carbon bond forming reactions, for example. The CSPVP can also be complexed with biomolecules such as proteins, DNA, and RNA, and used as nanocarriers for siRNA or dsRNA delivery.

专利号:US-2024124938-A1
优先权日:2019-10-16
标题:Visual detection of pbd induced dna crosslinks
发明人：LACHAUD CHRISTOPHE; COMBES SÉBASTIEN; ABEL SÉBASTIEN; AUDOLY GILLES; BERRADA SARA
权利人:INST NAT SANTE RECH MED; INST JEAN PAOLI & IRENE CALMETTES; AIX MARSEILLE UNIV; CENTRE NAT RECH SCIENT
摘要:The present invention relates to the field of oncology. laboratory tools and methods, and especially anti-tumor DNA crosslinking agents. Most patients with advanced solid tumors develop resistance to chemotherapy due to the ability of cancer cells to repair or tolerate sustained DNA damages. The inventors showed that the compounds according to the present invention allow the detection and visualization of alkylated DNA damages induced by PBDs without altering their DNA crosslinking ability. This enables the study of the effect and properties of PBDs. In particular, the present invention relates new derivates of PBD molecules and their synthesis. The present invention also relates to a method for visualizing DNA crosslinking: to a method for assessing the resistance of a tumor to a crosslinking agent and to a method for identifying a molecule or treatment for improving the efficiency of a crosslinking agent.

专利号:US-8987195-B2
优先权日:2012-08-08
标 题:HCV NS3 protease inhibitors
发明人：BARA THOMAS; BHAT SATHESH; BISWAS DIPSHIKHA; BROCKUNIER LINDA; BURNETT DUANE A; CHACKALAMANNIL SAMUEL; CHELLIAH MARIAPPAN V; CHEN AUSTIN; CLASBY MARTIN; COLANDREA VINCE J; GUO ZHUYAN; HAN YONGXIN; JAYNE CHARLES; JOSIEN HUBERT; MARCANTONIO KAREN; MIAO SHOUWU; NEELAMKAVIL SANTHOSH; PINTO PATRICK; RAJAGOPALAN MURALI; SHAH UNMESH; VELAZQUEZ FRANCISCO; VENKATRAMAN SRIKANTH; XIA YAN
权利人:MERCK SHARP & DOHME; MERCK CANADA INC
摘要:The present invention relates to hepatitis C virus (HCV) NS3 protease inhibitors containing a spirocyclic moeity, uses of such compounds, and synthesis of such compounds.

专利号:US-7256177-B2
优先权日:2003-06-17
标题 :Lincomycin derivatives possessing antibacterial activity
发明人：LEWIS JASON G; ANANDAN SAMPATH K; O'DOWD HARDWIN; GORDEEV MIKHAIL F
权利人:VICURON PHARM INC
摘要:Novel lincomycin derivatives are disclosed. These lincomycin derivatives exhibit antibacterial activity. The compounds of the subject invention may exhibit potent activities against bacteria, including Gram positive organisms, and may be useful antimicrobial agents. Methods of synthesis and of use of the compounds are also disclosed.