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Synthesis of stable isotope‐labeled metabolites of asenapine
Author(s) -
Kuethe Jeffrey T.
Publication year - 2012
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2924
Subject(s) - asenapine , chemistry , chemical synthesis , stable isotope ratio , glucuronide , combinatorial chemistry , metabolite , biochemistry , in vitro , lithium (medication) , medicine , physics , quantum mechanics , bipolar disorder , endocrinology
The stable isotope‐labeled synthesis of four of the major metabolites of asenapine is described. The synthesis of [ 13 CD 3 ]‐asenapine N ‐oxide proceeded in two synthetic steps. Preparation of [ 13 CD 3 ]‐asenapine 11‐hydroxysulfate and [ 13 C 6 ]‐ N ‐desmethylasenapine paralleled established synthetic protocols with effective utilization of labeled precursors. The synthesis of [ 13 CD 3 ]‐asenapine N + ‐glucuronide was achieved in three chemical steps followed by purification.