86232-34-0Relevant academic research and scientific papers
Approach to Merosesquiterpenes via Lewis Acid Catalyzed Nazarov-Type Cyclization: Total Synthesis of Akaol A
Kakde, Badrinath N.,Kumar, Nivesh,Mondal, Pradip Kumar,Bisai, Alakesh
, p. 1752 - 1755 (2016/05/19)
A Lewis acid catalyzed Nazarov-type cyclization of arylvinylcarbinol has been developed for the asymmetric synthesis of carbotetracyclic core of merosesquiterpenes. The reaction works only in the presence of 2 mol % of Sn(OTf)2 and Bi(OTf)3 in dichloroethane under elevated temperature. The methodology offers the synthesis of a variety of enantioenriched arylvinylcarbinols from commercially available (3aR)-sclareolide 9 in six steps with an eventual concise total synthesis of marine sesquiterpene quinol, akaol A (1a).
Design, Synthesis, and Biological Evaluation of Quercetagetin Analogues as JNK1 Inhibitors
Hierold, Judith,Baek, Sohee,Rieger, Rene,Lim, Tae-Gyu,Zakpur, Saman,Arciniega, Marcelino,Lee, Ki Won,Huber, Robert,Tietze, Lutz F.
, p. 16887 - 16894 (2015/11/16)
The recent discovery of c-Jun NH2-terminal kinase JNK1 suppression by natural quercetagetin (1) is a promising lead for the development of novel anticancer agents. Using both X-ray structure and docking analyses we predicted that 5′-hydroxy- (2
T-Bu2SiF-derivatized D2-receptor ligands: The first SiFA-containing small molecule radiotracers for target-specific PET-imaging
Iovkova-Berends, Ljuba,Waengler, Carmen,Zoeller, Thomas,Hoefner, Georg,Wanner, Klaus Theodor,Rensch, Christian,Bartenstein, Peter,Kostikov, Alexey,Schirrmacher, Ralf,Jurkschat, Klaus,Waengler, Bjoern
experimental part, p. 7458 - 7479 (2011/11/06)
The synthesis, radiolabeling and in vitro evaluation of new silicon-fluoride acceptor (SiFA) derivatized D2-receptor ligands is reported. The SiFA-technology simplifies the introduction of fluorine-18 into target specific biomolecules for Positron-Emission-Tomography (PET). However, one of the remaining challenges, especially for small molecules such as receptor-ligands, is the bulkiness of the SiFA-moiety. We therefore synthesized four Fallypride SiFA-conjugates derivatized either directly at the benzoic acid ring system (SiFA-DMFP, SiFA-FP, SiFA-DDMFP) or at the butyl-side chain (SiFA-M-FP) and tested their receptor affinities. We found D2-receptor affinities for all compounds in the nanomolar range (Ki(SiFA-DMFP) = 13.6 nM, Ki(SiFA-FP) = 33.0 nM, Ki(SiFA-DDMFP) = 62.7 nM and Ki(SiFA-M-FP) = 4.21 nM). The radiofluorination showed highest yields when 10 nmol of the precursors were reacted with [18F]fluoride/TBAHCO3 in acetonitrile. After a reversed phased cartridge purification the desired products could be isolated as an injectable solution after only 10 min synthesis time with radiochemical yields (RCY) of more than 40% in the case of SiFA-DMFP resulting in specific activities >41 GBq/μmol (>1,100 Ci/mmol). Furthermore, the radiolabeled products were shown to be stable in the injectable solutions, as well as in human plasma, for at least 90 min.
BENZENE COMPOUND AND SALT THEREOF
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Page 23, (2010/02/05)
The present invention provides a medicament comprising a benzene compound useful as an insulin sensitizer, a salt thereof or a hydrate of them and a derivative of them as the active ingredient. Specifically, it provides a benzene compound represented by t
CARBOXYLIC ACID DERIVATIVES AND DRUGS CONTAINING THE SAME
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, (2008/06/13)
The present invention provides a novel carboxylic acid compound, a salt thereof or a hydrate of them useful as an insulin-resistant improver, and a medicament comprising the compound as an active ingredient. That is, the present invention provides a carboxylic acid compound represented by the following formula (I), a salt thereof, an ester thereof or a hydrate of them. In the formula, R1 represents hydrogen atom, hydroxyl group or a C1-6 alkyl group etc. which may have one or more substituents; L represents a single or double bond or a C1-6 alkylene group etc. which may have one or more substituents; M represents a single bond or a C1-6 alkylene group etc. which may have one or more substituents; T represents a single bond or a C1-3 alkylene group which may have one or more substituents; W represents carboxyl group or a group represented by the formula -CON(Rw1)Rw2 (wherein Rw1 and Rw2 are the same as or different from each other and each represents hydrogen atom, formyl group etc.) etc.; represents a single or double bond; X represents oxygen atom or a C2-6 alkenylene group etc. which may have one or more substituents; Y represents a C5-12 aromatic hydrocarbon group etc. which may have one or more substituents and which may have one or more heteroatoms; and ring Z represents a C5-6 aromatic hydrocarbon group which may have 0 to 4 substituents and which may have one or more heteroatoms.
SYNTHESIS OF 5-HALOGEN-SUBSTITUTED 2,3-DIHYDROXYPHENYLACETIC ACIDS, THEIR ESTERS, AND 2,3-DIMETHOXYPHENYLACETOHYDROXAMIC ACIDS
Daukshas, V. K.,Martinkus, R. S.,Kuleshyus, V. A.,Shtel'bene, V. P.
, p. 458 - 463 (2007/10/02)
Many-stage general methods were developed for the synthesis of 5-bromo- or 5-chloro-substituted 2,3-dimethoxyphenylacetic acids from o-vanilin.Methods were also developed for their conversion into the corresponding hydroxamic acids, 2,3-dihydroxyphenylace
