124391-76-0Relevant articles and documents
A rapid and convenient synthesis of β-proline
Blanchet, Jér?me,Pouliquen, Mickael,Lasne, Marie-Claire,Rouden, Jacques
, p. 5727 - 5730 (2008/02/09)
A short, reliable, and cheap synthesis of both enantiomers of β-proline, an efficient organocatalyst and an important building block in medicinal chemistry, has been developed in four steps (overall yield: 72%) from the diasteromeric adducts of methyl itaconate and (R)-α-methylbenzylamine. The key step involves the chemoselective reduction of a lactam group in the presence of a benzyl ester.
Ligands for monoamine receptors and transporters, and methods of use thereof
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, (2008/06/13)
One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.
CHIRAL SYNTHESIS VIA ORGANOBORANES. 19. THE SUCCESSFUL ONE-CARBON HOMOLOGATION OF HETEROCYCLIC BORONATE ESTERS WITH HIGH OPTICAL PURITY
Brown, Herbert C.,Gupta, Ashok K.,Rangaishenvi, Milind V.,Vara Prasad, J. V. N.
, p. 283 - 294 (2007/10/02)
An exploratory study was undertaken to establish the applicability of the one-carbon homologation to heterocyclic boronic esters.This procedure involves the use of (cloromethyl)lithium, LiCH2Cl, generated in situ by the reaction of bromochloromethane and n-BuLi in THF at -78 deg C in the presence of an enantiomerically pure heterocyclic boronic ester.These heterocyclic boronic esters were prepared via asymmetric hydroboration of representative heterocyclic olefins bearing either an endocyclic or exocyclic double bond with either Ipc2BH or IpcBH2 in THF.