Discovery of novel non-peptidic β-alanine piperazine amide derivatives and their optimization to achiral, easily accessible, potent and selective somatostatin sst1 receptor antagonists
摘要:
Structural simplification of the core moieties of obeline and ergoline somatostatin sst(1) receptor antagonists, followed by systematic optimization, led to the identification of novel, highly potent and selective sst(1) receptor antagonists. These achiral, non-peptidic compounds are easily prepared and show promising PK properties in rodents. (C) 2009 Elsevier Ltd. All rights reserved.
the presence of manganese(III) acetate gives naphthalenecarbaldehydes and naphthalenecarboxylic acids. Similar reactions of anthracene, pyrene, and methoxybenzenes also yield formylated and carboxylated products. It was found that the formyl group introduced to the aromatic ring was not derived from carboxymethyl radical generated directly by the thermolysis of manganese(III) acetate, but from a dicarboxymethyl
The invention relates to an image support medium for creation of an aesthetic image that is an work or object for display. This support medium includes a polymer in an amount sufficient to enable the image to have at least one aesthetic element. In different embodiments, the image support medium is an image support stabilizer, the polymer is a synthetic absorbent or conductive polymer, or the polymer is a transparent or synthetic translucent polymer and a property of this transparent or translucent polymer is enhanced to facilitate the creation or preservation of the image by at least one stabilizer. The invention also relates to a method for preparing this image support medium. The method includes forming a reaction mixture comprising a monomer in an amount sufficient to provide or enable the image to have an aesthetic element, and processing the reaction mixture into a 2- or 3-dimensional shape.
Oxidation of xanthenes with manganese(III) acetate in the presence of active methylene compounds such as 1,3-dicarbonyl compounds, malononitrile derivatives, acetone, and nitromethane selectively gives 9-substituted xanthene derivatives in good yields. A similar oxidation of thioxanthene also yields 2-(9-thioxanthenyl)-1,3-dicarbonyl compounds in 57-91% yields. The obtained 2-(9-xanthenyl)-1,3-dicarbonyl compounds are readily converted to 2-(9-xanthenylidene)-1,3-dicarbonyl derivatives using manganese(III) complexes or 2,3-dichloro-5, 6-dicyano-1,4-benzoquinone. The mechanisms for the formation of 9-substituted xanthenes are discussed on the basis of the reaction of intermediates, the electron-donating substituent effect on the xanthene ring system, effect of additives, and comparison with a reaction of radical-trapping reagents.
Fosse, Bulletin de la Societe Chimique de France, 1906, vol. <3> 35, p. 1005
作者:Fosse
DOI:——
日期:——
Fosse, Annales de Chimie (Cachan, France), 1920, vol. <9> 13, p. 106