- AZABICYCLO AND DIAZEPINE DERIVATIVES FOR TREATING OCULAR DISORDERS
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The present invention provides in one aspect azabicycio and diazepine derivatives useful as modulators of muscarinic receptors. In another aspect, the present invention provides pharmaceutical compositions for treating ocular diseases, the compositions comprising at least one muscarinic receptor modulator. Formulae (I) & (II):
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- Aziridination of alkenes using 3-acetoxyamino-2-trifluoromethylquinazolin-4(3H)-one
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Oxidation of 3-amino-2-trifluoromethylquinazolin-4(3H)-one 6 with lead tetraacetate in dichloromethane gives the title 3-acetoxyamino derivative 7 which is isolable at room temperature and considerably more stable than the corresponding 2-alkyl substituted analogues. Compound 7 aziridinates alkenes in yields which are consistently higher than those from the 2-alkyl substituted analogues. Aziridinations using 3-acetoxyaminoquinazolinones bearing other electron-withdrawing groups on the 2-position of the quinazolinone ring have been examined.
- Atkinson, Robert S.,Coogan, Michael P.,Cornell, Clive L.
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p. 157 - 166
(2007/10/03)
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- The in situ generation and trapping of some fluorine-substituted ketenes
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Fluoroketene, difluoroketene, methylfluoroketene, trifluoromethylfluoroketene, and phenylfluoroketene were each generated, in situ, via dehydrohalogenation of the respective acid chlorides. In the presence of cyclopentadiene [2 + 2] adducts were obtained in all but the difluoroketene case. In the absence of cyclopentadiene, low temperature 19F nmr indicated the presence of acyl ammonium salts and enolates, potential precursors of the ketenes, but no actual ketene species could unambiguously be detected. The stereochemical results were consistent with the currently accepted steric-based mechanistic rationale for stereochemical determination in ketene cycloadditions.
- Dolbier Jr., William R.,Lee, Suk Kyu,Phanstiel IV, Otto
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p. 2065 - 2072
(2007/10/02)
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