7176-39-8Relevant articles and documents
A Bioinspired Synthesis of Polyfunctional Indoles
Huang, Zheng,Kwon, Ohhyeon,Huang, Haiyan,Fadli, Aziz,Marat, Xavier,Moreau, Magali,Lumb, Jean-Philip
supporting information, p. 11963 - 11967 (2018/09/11)
Polyfunctional indoles bearing substituents at C5 and C6 are prevalent in natural products, pharmaceuticals, agrochemicals, and materials. Owing to the remoteness of the C5 and C6 positions, indoles of this family can be difficult to prepare, and often require multistep syntheses. Herein, we describe a concise process that converts simple derivatives of tyrosine into 5,6-difunctionalized indoles by direct oxidation of C?H, N?H, and O?H bonds. Our work draws inspiration from the biosynthetic polymerization of tyrosine to make melanin pigments, but makes an important departure to provide well-defined indole heterocycles.
DERIVATIVES OF 4-(2-AMINO-1-HYDROXYETHYL)PHENOL AS AGONISTS OF THE BETA2 ADRENERGIC RECEPTOR
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Page/Page column 20, (2009/07/03)
The present invention provides a compound of formula (I): wherein: ? R1 is a group selected from -CH2OH,-NH(CO)H and ? R2 is a hydrogen atom; or ? R1together with R2 form the group -NH-C(O)-CH=CH-, wherein the nitrogen atom is bound to the carbon atom in the phenyl ring holding R1and the carbon atom is bound to the carbon atom in the phenyl ring holding R2 ? R3a and R3bare independently selected from the group consisting of hydrogen atoms and C1-4alkyl groups, ? n represents an integer from 1 to 3; ? Ad represents 1-adamantyl or 2-adamantyl group, or a pharmaceutically-acceptable salt or solvate or stereoisomer thereof.
Synthesis and preliminary evaluation of (R,R)(S,S) 5-(2-(2-[4-(2-[18F]fluoroethoxy)phenyl]-1-methylethylamino)- 1-hydroxyethyl)-benzene-1,3-diol ([18F]FEFE) for the in vivo visualisation and quantification of the β2-adrenergic receptor status in lung
Schirrmacher, Esther,Schirrmacher, Ralf,Thews, Oliver,Dillenburg, Wolfgang,Helisch, Andreas,Wessler, Ignatz,Buhl, Roland,Hoehnemann, Sabine,Buchholz, Hans-Georg,Bartenstein, Peter,Machulla, Hans-Juergen,Roesch, Frank
, p. 2687 - 2692 (2007/10/03)
The 18F-labeled β2-adrenergic receptor ligand (R,R)(S,S) 5-(2-(2-[4-(2-[18F]fluoroethoxy)phenyl]-1-methylethylamino)- 1-hydroxyethyl)-benzene-1,3-diol, a derivative of the original highly selective racemic fenoterol, was synthesized in an overall radiochemical yield of 20% after 65 min with a radiochemical purity higher than 98%. The specific activity was in the range of 50-60 GBq/μmol. In vitro testing of the non-radioactive fluorinated fenoterol derivative with isolated guinea pig trachea was conducted to obtain an IC50 value of 60 nM. Preliminary ex vivo organ distribution and in vivo experiments with positron emission tomography (PET) on guinea pigs were performed to study the biodistribution as well as the displacement of the radiotracer to prove specific binding to the β2-receptor.