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ESR studies on the radical cation mechanism of the ring opening of cyclopropylamines

Journal Article · · J. Am. Chem. Soc.; (United States)
DOI:https://doi.org/10.1021/ja00236a055· OSTI ID:6970253

Cyclopropylamine radical cations have been implicated in the mechanism of inactivation of monoamine oxidase and cytochrome P-450 by cyclopropylamines. The key step in the proposed mechanism is illustrated for the parent compound in Scheme I and consists of the ring opening of the aminium radical cation 1 to the carbon-centered radical 2 which subsequently attacks the active site of the enzyme. Here they present ESR evidence for this ring-opening reaction and report that 2 is not converted to the nitrogen-centered radical 3 whereas the corresponding reaction for the neutral radical proceeds to completion at similar temperatures. These results provide a firm basis for the radical cation mechanism of enzyme inactivation, in keeping with the structural evidence that the inactivator is bound to the enzyme through carbon rather than nitrogen.

Research Organization:
Univ. of Tennessee, Knoxville
OSTI ID:
6970253
Journal Information:
J. Am. Chem. Soc.; (United States), Journal Name: J. Am. Chem. Soc.; (United States) Vol. 109:2; ISSN JACSA
Country of Publication:
United States
Language:
English