Synthesis of stable isotope‐labeled metabolites of asenapine
Authors:
Jeffrey T. Kuethe
Affiliation:
Department of Process Research, Labeled Compound Synthesis Group, Merck & Co., Inc., , Rahway, NJ, 08065 USA
Abstract:
The stable isotope‐labeled synthesis of four of the major metabolites of asenapine is described. The synthesis of [13CD3]‐asenapine N‐oxide proceeded in two synthetic steps. Preparation of [13CD3]‐asenapine 11‐hydroxysulfate and [13C6]‐N‐desmethylasenapine paralleled established synthetic protocols with effective utilization of labeled precursors. The synthesis of [13CD3]‐asenapine N+‐glucuronide was achieved in three chemical steps followed by purification.