The synthesis and biological activity of some known and putative metabolites of the atypical antipsychotic agent olanzapine (LY170053)

4′-N-desmethyl olanzapine (2), olanzapine 4′-N-oxide (3) and 2-hydroxymethyl olanzapine (5), have been prepared and their pharmacology compared to that of the parent compound olanzapine (1). The 4′-N-quaternary glucuronide (8) has also been prepared.