Syntheses of the tricyclic cores of clozapine, dibenzo[b,f][1,4]thiazepin-11(10H)-one, and dibenzo[b,f][1,4]oxazepin-11(10H)-one in C-14 labeled form by [14C]carbonylation
作者： Charles S. Elmore , Peter N. Dorff , J. Richard Heys
DOI: 10.1002/JLCR.1802
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摘要: Clozapine has been demonstrated to bind covalently proteins as a result of metabolic activation that proposed be precursor the serious side effects including death occur in small percentage population. The covalent modification by clozapine studied several groups and is well documented; therefore, department drug metabolism desired use [14C]clozapine positive control for binding assays. preparation was first conducted using previous reported route then new utilized [14C]carbonylation isotope incorporating step. While this worked, it not deemed superior route. However, methodology proved quite effective preparing C-14 labeled dibenzothiazepine dibenzoxapine ring systems. Copyright © 2010 John Wiley & Sons, Ltd.
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