Design, Synthesis, and Evaluation of 5′-Diphenyl Nucleoside Analogues as Inhibitors of the Plasmodium falciparum dUTPase
作者:Shahienaz E. Hampton、Beatriz Baragaña、Alessandro Schipani、Cristina Bosch-Navarrete、J. Alexander Musso-Buendía、Eliseo Recio、Marcel Kaiser、Jean L. Whittingham、Shirley M. Roberts、Mikhail Shevtsov、James A. Brannigan、Pia Kahnberg、Reto Brun、Keith S. Wilson、Dolores González-Pacanowska、Nils Gunnar Johansson、Ian H. Gilbert
DOI:10.1002/cmdc.201100255
日期:2011.10.4
Deoxyuridine 5'-triphosphate nucleotidohydrolase (dUTPase) is a potential drug target for malaria. We previously reported some 5'-tritylated deoxyuridine analogues (both cyclic and acyclic) as selective inhibitors of the PlasmodiumfalciparumdUTPase. Modelling studies indicated that it might be possible to replace the trityl group with a diphenyl moiety, as two of the phenyl groups are buried, whereas
A method for preparing
18
F-BPA and an intermediate, by which high-purity
18
F-BPA is obtained. The method simplifies the synthesis steps after
18
F labeling, and is easy to operate and efficient.
4-Methoxy-Pyrrolidine-2-Carboxylic Acid Compounds and Derivatives Thereof as Hepatitis C Virus Inhibitors
申请人:Guidetti Rossella
公开号:US20070270475A1
公开(公告)日:2007-11-22
Anti-viral agents of Formula (Ia)
wherein: A represents hydroxy; D represents 4-tert-butyl-3-methoxyphenyl; E represents 1,3-thiazol-2-yl or 5-methyl-1,3-thiazol-2-yl,; G represents methoxymethyl; J represents 1,3-thiazol-2-ylmethyl, 1,3-thiazol-4-ylmethyl, 1,2-thiazol-3-ylmethyl, or 1H-pyrazol-1-ylmethyl; and salts, solvates and esters thereof; provided that when A is esterified to form —OR where R is selected from straight or branched chain alkyl, aralkyl, aryloxyalkyl, or aryl, then R is other than tert-butyl; processes for their preparation and their use in HCV treatment are provided.
Disclosed herein is a process for preparing a compound of Formula (I), comprising the steps of: (a) reacting an aniline compound of Formula (II) and an carboxylic acid compound of Formula (III) or an activated carboxylic acid compound thereof, to provide a compound of Formula (IV); and (b) converting said protected amine group attached to said compound of Formula (IV) to an amine group to provide said compound of Formula (I); wherein PAm is a protected amine group. Processes to prepare the compounds of Formulae (II), (III), and (IV) are also disclosed.
Disclosing Cyclic(Alkyl)(Amino)Carbenes as One‐Electron Reductants: Synthesis of Acyclic(Amino)(Aryl)Carbene‐Based Kekulé Diradicaloids
作者:Avijit Maiti、Benedict J. Elvers、Sachinath Bera、Felix Lindl、Ivo Krummenacher、Prasanta Ghosh、Holger Braunschweig、Cem B. Yildiz、Carola Schulzke、Anukul Jana
DOI:10.1002/chem.202104567
日期:2022.5.16
Herein, we disclose cyclic(alkyl)(amino)carbenes (CAACs) to be one-electron reductants under the formation of a transient radical cation as indicated by EPR spectroscopy. The disclosed CAAC reducing reactivity was used to synthesize acyclic(amino)(aryl)carbene-based Thiele and Chichibabin hydrocarbons, a new class of Kekulé diradicaloids. The results demonstrate CAACs to be potent organic reductants