900535-40-2Relevant academic research and scientific papers
Highly enantioselective access to α-dibenzylamino ketones from chiral nonracemic α-bromo α′-sulfinyl ketones by dynamic kinetic resolution: Synthesis of (2R,1′S)-2-[1-(dibenzylamino)alkyl]oxiranes
Geant, Pierre-Yves,Martinez, Jean,Salom-Roig, Xavier J.
experimental part, p. 1300 - 1309 (2011/04/17)
A novel and efficient synthesis of enantiomerically pure α-dibenzylamino α′-sulfinyl ketones starting from a mixture of both epimers of α-bromo α′-(R)-sulfinyl ketone has been realized through combined in situ substitution-epimerization in a so-called Dynamic Kinetic Resolution (DKR). The scope of the reaction has been examined, and four differently substituted α-(S)-dibenzylamino α′-(R)- sulfinyl ketones were obtained in good yields with excellent diastereoselectivities. The utility of these derivatives was further illustrated with a highly stereoselective synthesis of syn-(2R,1′S)-2-(1- dibenzylaminoalkyl)oxiranes.
PYRIDAZINONE GLUCOKINASE ACTIVATORS
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Page/Page column 45, (2009/10/30)
Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.
Privileged structure based ligands for melanocortin-4 receptors-Aliphatic piperazine derivatives
Briner, Karin,Collado, Iván,Fisher, Matthew J.,García-Paredes, Cristina,Husain, Saba,Kuklish, Steven L.,Mateo, Ana I.,O'Brien, Thomas P.,Ornstein, Paul L.,Zgombick, John,de Frutos, óscar
, p. 3449 - 3453 (2007/10/03)
Aliphatic carbocyclic replacement of the benzyl group of compound 1 yielded compounds with high affinity for the melanocortin-4 receptor (MC4R). Compounds with a cyclohexyl group showed a consistent high affinity, while different polar groups with less basicity were good replacements for the original diethyl amines. Substitution of the polar group found in these privileged structures with an aliphatic moiety produced compounds with high affinity for MC4R.
