439614-60-5Relevant academic research and scientific papers
Redox-Neutral Manganese(I)-Catalyzed C?H Activation: Traceless Directing Group Enabled Regioselective Annulation
Lu, Qingquan,Gre?ies, Steffen,Cembellín, Sara,Klauck, Felix J. R.,Daniliuc, Constantin G.,Glorius, Frank
, p. 12778 - 12782 (2017/09/11)
A strategy is reported in which traceless directing groups (TDGs) are used to promote the redox-neutral MnI-catalyzed regioselective synthesis of N-heterocycles. Alkyne coupling partners bearing a traceless directing group, which serves as both the chelator and internal oxidant, were used to control the regioselectivity of the annulation reactions. This operationally simple approach is highly effective with previously challenging unsymmetrical alkyne systems, including unbiased dialkyl alkynes, with perfect regioselectivity. The simple conditions and the ability to carry out synthesis on a gram scale underscore the usefulness of this method. The application of this strategy in the concise synthesis of the bioactive compound PK11209 and the pharmaceutical moxaverine is also described.
1-(Phenyl)isoquinoline carboxamides: A novel class of subtype selective inhibitors of thyrotropin-releasing hormone (TRH) receptors
Jiang, Jian-Kang,Thomas, Craig J.,Neumann, Susanne,Lu, Xinping,Rice, Kenner C.,Gershengorn, Marvin C.
, p. 733 - 736 (2007/10/03)
We report the synthesis of and binding to the two subtypes of mouse thyrotropin-releasing hormone (TRH) receptors, TRH-R1 and TRH-R2, of several 1-(phenyl)isoquinoline carboxamide analogues. These analogues showed a degree of selectivity for binding at TR
Multi-use multimodal imaging chelates
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, (2008/06/13)
Cyclen-based chelates can be used as contrast agents for multi-modal imaging of tissue cells. The cyclen-based chelates are preferably polyazamacrocyclic molecules formed from 1,4,7,10 tetraazacyclododecane (“cyclen”) having varying chelating ions, phosphoester chains, and light harvesting moieties. By changing the chelating ion, phosphoester chain length and/or the light harvesting moiety different imaging techniques, such as MRI, CT, fluorescence and absorption, x-ray and NIR, may be employed to image the tissue cells. Additionally, the cyclen-based chelates may be conjugated to provide for site-specific delivery of the cyclen-based chelate to the desired tissue cells. The cyclen-based chelates may also be delivered to the tissue cells by attaching the cyclen-based chelates to a polymeric delivery vehicle. Although these cyclen-based chelates have a wide variety of application, the preferred use is for imaging of cancer cells, such as brain cancer, for improving resection of a cancerous tissue.
Synthetic approaches to 1-(2-chlorophenyl)isoquinoline-3-carboxylic acid
Janin, Yves L.,Roulland, Emmanuel,Beurdeley-Thomas, Arnaud,Decaudin, Didier,Monneret, Claude,Poupon, Marie-France
, p. 529 - 532 (2007/10/03)
In connection with our research of new antitumor compounds, previously undescribed approaches to the 1-(2-chlorophenyl)isoquinoline-3-carboxylic acid 9 are reported here. Two related accesses from phenylethylamine or amphetamine were investigated and were found to be successful. A more robust synthesis, using Suzuki's cross-coupling between 2-chlorophenylboronic acid 15 and the previously unreported methyl-1-bromoisoquinoline-3-carboxylate 14 was also developed. This synthetic route provides the ground for a combinatorial approach to the core structure of new potential peripheral benzodiazepine receptor ligands.
Facile, Efficient Conjugation of a Trifunctional Lanthanide Chelate to a Peripheral Benzodiazepine Receptor Ligand
Manning, H. Charles,Goebel, Timothy,Marx, John N.,Bornhop, Darryl J.
, p. 1075 - 1077 (2007/10/03)
matrix presented Receptor-mediated imaging and therapy of diseased tissue is rapidly gaining favor in the medical community. The synthesis and facile aqueous/ organic coupling of a peripheral-type benzodiazepine receptor ligand to a cyclen-based fluoropho
