Thermally induced opening of the diaziridine ring in 6-aryl-2-methyl-1,5- diazabicyclo[3.1.0]hexanes
Thermally induced opening of the diaziridine ring in 6-aryl-2-methyl-1,5- diazabicyclo[3.1.0]-hexanes at the carbon-nitrogen bond is characterized by low regioselectivity; isomerization of unstable intermediate azomethine imines leads to mixtures of the corresponding 1-arylmethyl-5-methyl-4,5-dihydro-1H-pyrazoles and 1-arylmethyl-3-methyl-4,5-dihydro-1H-pyrazoles at a ratio of ~6:5. Analogous regioselectivity in opening of the three-membered ring is observed in the presence of phenyl isocyanate. In this case, adducts with cis arrangement of the aryl and methyl groups are formed as the major products (cis/trans ratio ~3:1).
Method of optically resolving (±)-1-(3-pyridylcarbonyl)-5-methyl-2-pyrazoline
The present invention relates to a novel (-)-2-pyrazoline compound and therapeutic agents containing the same as an effective ingredient; furthermore, it relates to a method for optically resolving 1-(3-pyridylcarbonyl)-5-methyl-2-pyrazoline.
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(2008/06/13)
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