CAS: 84348-37-8; Boc-4-Oxo-Pro-Oh

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L-羟基脯氨酸置于jones Reagent,Sodium Carbonate体系中,用 四氢呋喃,1,4-二氧六环,水,丙酮 作为反应溶剂,化学反应 22.58H,反应生成 N-Boc-4-氧代-脯氨酸
参考文献:化学探针揭示了由人类阿片强啡肽与细菌传感器激酶结合引发的抗菌防御反应
标题:化学探针揭示了由人类阿片强啡肽与细菌传感器激酶结合引发的抗菌防御反应
摘要:通过小分子信号进行宿主-微生物交流对于共生和致病关系都很重要,但在分子水平上往往知之甚少.在宿主压力条件下,人阿片肽强啡肽的水平升高,通过未知途径触发机会致病菌铜绿假单胞菌的毒力.在这里,我们应用多层化学生物学策略来揭示这种假定的界际信号的作用模式.我们设计并应用了强啡肽启发的光亲和探针,通过化学蛋白质组学揭示活细菌中肽的蛋白质靶标.pars 是一种基本上没有特征的双组件系统膜传感器,被认为是最有希望的产品.随后的完整蛋白质组研究表明,强啡肽 (1-13) 在假单胞菌中诱导抗菌肽样反应,并特异性上调膜防御机制.在 Pars 突变体中没有观测到这种反应,它对强啡肽诱导的毒性更敏感.因此,铜绿假单胞菌利用 Pars 传感机制来防御宿主以响应强啡肽作为信号.这项研究强调界际交流是一种潜在的基本策略,不仅可以诱导铜绿假单胞菌的毒力,而且可以在宿主的恶劣环境中维持生存能力.铜绿假单胞菌利用 Pars
DOI:10.1021/jacs.7B01072

专利信息

专利号:US-8927739-B2
优先权日:2011-05-18
标 题 :Processes for the preparation of 5-azaspiro[2.4]heptane-6-carboxylic acid and its derivatives
发明人：QIU YAO-LING; PENG XIAOWEN; KIM IN JONG; CAO HUI; TANG DATONG; OR YAT SUN; WANG GUOQIANG; XU GUOYOU
权利人:ENANTA PHARM INC
摘要:The present invention relates generally to an improved process for the preparation of 5-azaspiro[2.4]heptane-6-carboxylic acid and its derivatives which are useful intermediates in the synthesis of biologically active molecules, especially in the synthesis of hepatits C virus NS5A inhibitors. In particular, the present invention relates to processes and intermediates for the preparation of compounds of formulae (Ia), (Ib) and (Ic):

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-11472838-B2
优先权日:2018-04-17
标 题:Inhibitors of blood coagulation factor XIII
发明人：HILS MARTIN; PASTERNACK RALF; BÃœCHOLD CHRISTIAN
权利人:ZEDIRA GMBH
摘要:The invention relates to a compound of general formula (I) as novel inhibitor of blood coagulation factor XIII, methods for synthesis thereof and to use thereof for the prophylaxis or treatment of diseases associated with blood coagulation factor XIII.

专利号:US-6642264-B1
优先权日:1999-04-06
标 题 :Thiazolobenzoimidazole derivatives
发明人：HAYASHIBE SATOSHI; ITAHANA HIROTSUNE; OKADA MASAMICHI; KOHARA ATSUYUKI; MAENO KYOICHI; YAHIRO KIYOSHI; SHIMADA ITSURO; TANABE KAZUHITO; NEGORO KENJI; KAMIKUBO TAKASHI; SAKAMOTO SHUICHI
权利人:YAMANOUCHI PHARMA CO LTD
摘要:This invention relates to novel thiazolo[3,2-a]benzoimidazole derivatives represented by the following general formula (I). The compounds provided by the invention act specifically on metabotropic glutamate receptors and are used as medicaments. The invention also provides novel compounds useful as intermediates for the synthesis of the compounds of the invention.(Symbols in the formula represent the following meanings. R<1>: carbamoyl, carbonyl, oxy, amino, carbonylamino or the like which may be substituted; R<2>: hydrogen, lower alkyl or the like; and R<3>, R<4 >and R<5>: hydrogen, lower alkyl and the like which may be the same or different from one another.)

专利号:IT-UB20152779-A1
优先权日:2015-08-03
标题 :PROCESS FOR THE SYNTHESIS OF 4-PROTECTED CHETO PROLINA

专利号:US-7199105-B2
优先权日:2002-08-15
标 题:Lincomycin derivatives possessing antibacterial activity
发明人：LEWIS JASON G; PATEL DINESH V; ANANDAN SAMPATH KUMAR; GORDEEV MIKHAIL F
权利人:VICURON PHARM INC
摘要:Novel lincomycin derivatives are disclosed. These lincomycin derivatives exhibit antibacterial activity. As the compounds of the subject invention exhibit potent activities against bacteria, including gram positive organisms, they are useful antimicrobial agents. Methods of synthesis and of use of the compounds are also disclosed.