31559-00-9Relevant articles and documents
SUBSTITUTED DIHYDRO AND TETRAHYDRO OXAZOLOPYRIMIDINONES, PREPARATION AND USE THEREOF
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Page/Page column 27, (2010/04/23)
The present invention relates to a series of substituted dihydro and tetrahydro oxazolopyrimidinones, specifically, to a series of 2-substituted-2,3-dihydro-oxazolo[3,2-a]pyrimidin-7-ones and 2-substituted-2,3,5,6-tetra-hydro-oxazolo[3,2-a]pyrimidin-7-ones of formula (I): Wherein p, n, X, Y, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein. This invention also relates to methods of making these compounds including novel intermediates. The compounds of this invention are modulators of metabotropic glutamate receptors (mGluR), particularly, mGluR2 receptor. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic neurodegenerative conditions, psychoses, convulsions, anxiety, depression, migraine, pain, sleep disorders and emesis.
THE EFFECTS OF SUBSTITUENS AND SOLVENT POLARITY ON PHOTOCHEMICAL SIGMATROPIC SHIFTS. EXPERIMENTAL EVIDENCE IN FAVOUR OF THE OCCURRENCE OF SUDDEN POLARIZATION IN ACYCLIC ALKENES
Peijnenburg, W. J. G. M.,Buck, H. M.
, p. 4927 - 4940 (2007/10/02)
Furher experimental evidence regarding the occurence of sudden polarization in acyclic alkenes is presented.It is shown that the yield of formation of the product derived from an intramolecular photochemical -OH shift in the 1 is dependent only on the polarity of the solvent employed.This result could be well explained in terms of a stabilization of the zwitterionic intermediate formed upon irradiation of 1 by reorientation polarization of the dipole solvent molecules.Besides this, it was found that replacement of the alkyl group at the terminal carbon atom of the C3-C9 exocyclic double bond in 1 by a phenyl substituent led to the occurence of a photochemical -H shift.This directive effect of the substituents at the exocyclic double bond could be well explained on the basis of the sudden polarization model.